Perspective on Chemist’s Tool Box Towards Synthesis of

Anti-tubercular Agents
Prof. Anamik Shah, Vice Chancellor, Gujarat Vidyapith, Ahmedabad – 380014.

Resurgence of Tuberculosis, especially drug resistance by Mycobacterium

Tuberculosis has posed a great threat to mankind& it is now at ever alarming stage. There is a
need for working on new drug discovery by more innovative ways in compare to efforts done
is past. Identification of now leads and drugs is a herculean task. The present talk will give an
overview of two decade of a collaborative work done by our research team involving design,
synthesis, biological screening, use of bioinformatic tools & redesigning of some potential
lead to arrive at some promising patented molecules.
 Visualizing the structures of biological macromolecules
M.R.N. Murthy, Molecular Biophysics Unit, Indian Institute of Science, Bengaluru 560012

Awareness of the existence of a vast microbial world inaccessible to our naked eyes
but of crucial importance for our health had to await development of optical microscopes.
Optical microscopes, however powerful, cannot reveal structures smaller than the wavelength
of light used for imaging. Even the largest of biomolecules are much smaller than the
wavelength of visible light that ranges between 400 nm and 800 nm. About a hundred years
ago, X-ray diffraction, the phenomenon of scattering of X-radiation is specific directions by
crystallize substances, was shown to have the power of revealing the atomic structure of
molecules constituting the crystal. Over the century, the technique was developed into a
powerful tool to visualize the structure of small organic molecules as well as large
biomolecules. This field has revolutionized our understanding of chemistry and biology by
allowing us to determine the atomic structure of hundreds of thousands of molecules.
However, the technique needs crystals of the material or molecule whose structure needs to
be determined. It cannot be applied to molecules in solution. Another method that has
become recently available is cryo-electron microscopy. In 1924, the French physicist de
Broglie suggested that electrons, till then considered as particles circling atomic nuclei, could
also possess wave like properties. The wavelength associated with electrons depends on their
momentum (or velocity). Ruska and Knowl succeeded in constructing the first microscope
that used electron waves in 1932. In the electron microscope, electro magnets act as lenses
and bend or focus the electron waves. In the "negative staining technique" of viewing
biological molecules by electron microscopy, the sample is dehydrated (dried) and stained
with a heavy atom salt. This distorts the molecule constituting the sample and limits the
resolution of the images. To keep the samples hydrated and preserve the native structure of
biomolecules, cryo-electron microscopy that operates in the temperature range of -130 to -
180o C was developed. The images recorded in the microscope represent two dimensional
projections. Methods were developed to obtain three-dimensional structural information
using two dimensional projections. With these developments, cryo-electron microscopy has
become an extremely powerful tool for studying biomolecular structure and function. The
lecture will present these two techniques and their enormous impact on modern biology.
 PERSPECTIVES AND CHALLENGES IN DRUG RESEARCH
P.M.S.Chauhan
Chief Scientist Medicinal and Process Chemistry Division, Central Drug Research Institute Lucknow, India
226001Email;[email protected],[email protected],

Nitrogen heterocycles are constituted a major class of existing drugs. These

compounds are widely distributed in nature and are essential to life
process.They also play a vital role in the controlling the metabolism of all living
cells. The activity of these molecules is attributed to their ability to interfere
against several important biological target sites. Keeping in view importance of
nitrogen hetrocycles in antiparasitic area, we have synthesized novel
heterocycles. These heterocycles were synthesized by classical solution phase as
well as on solid support. Several synthesized compounds have shown promising
in vitro and in vivoantiparasitic activity against Malaria and
Leshimaniaparasites.The design, synthesis and antiparasitic activity of these
novel antiparasitic agents will be discussed
 Designing of templates to reach the distal C–H bond
Debabrata Maiti
Department of Chemistry, Indian Institute of Technology Bombay, India.
E-mail: [email protected]

Abstract:

Mimicking the nature has always been a coveted target for scientific communinities.
A precise understanding has emerged as to how enzymes accomplish the chemical
transformations. Enzymes catalyze inert C-H bond functionalization in a regio- and
stereoselctive manner using metal-active site. Inspired by the nature, we have developed
catalytic methods to functionalize carbon–hydrogen (C–H) bonds which provides significant
economic and environmental benefits over traditional synthetic methods. Applicability of our
strategies towards synthesis of various complex molecules will be discussed.

References:

1. Deb, A.; Bag, S.; Kancherla, R.; Maiti, D. J. Am. Chem. Soc.2014, 136, 13602-13605.
2. Bera, M.; Maji, A.; Sahoo, S. K.; Maiti, D. Angew. Chem. Int. Ed.2015, 54, 8515–8519.
3. Bag, S.; Patra, T.; Modak, A.; Deb, A… Bera, M.; Maiti, D. J. Am. Chem. Soc. 2015, 137, 11888–11891.
4. Patra, T.; Bag, S.; Kancherla, R… Modak, A.; Maiti, D. Angew. Chem. Int. Ed.2016, 55, 7751–7755.
5. Bag, S.; Jayarajan, R.; Dutta, U.; Chowdhury, R.; Mondal, R.; Maiti, D. Angew. Chem. Int. Ed.2017, 56, 12538–12542.
 “Role of metal ions in Mycobacterial DNA damage response”
Saravanan Matheshwaran *
Department of Biological Sciences and Bioengineering
Indian Institute of Technology – Kanpur, Uttar Pradesh
* Contact: Email: [email protected] ; Phone: 0512 259 4066

One of the major challenges being faced in the control of TB is the increased advent of
multidrug resistant forms of the pathogen. Usually the treatment of TB is prolonged since the
pathogen enters into a latent state protected by a structure known as the granuloma. Within
the granuloma the pathogen encounters a hostile environment rendering it prone to DNA
damage. In MTB, SOS response is one of the essential systematic mechanisms against stress.

During stress conditions, the levels of metal ions concentration within the cell is altered and
suggested to be have role in stress response. However, the exact roles for the metal ions are
not yet clear in MTB SOS response.

Metal ions are known to stabilize, destabilize, or modulate biological molecules by

introducing conformational changes and by creating centers of activity in the
biomacromolecule. The distribution of these metals in the cell as a function of time and
location is critical for the regulation of various biological processes. Here we will be
presenting two unreported roles for metal ions in proteins that participate in mycobacterial
DNA damage response.
 Chemo-Catalytic Avenues for Bio-Refinery Applications
C. V. Rode
CEPD Division, CSIR-National Chemical Laboratory, Pune 411008
[email protected]

Crude oil which is a diminishing feed stock has been the source of fuel and synthetic materials of the
modern society. A step forward towards achieving sustainability and reduction in carbon footprints is
the realization of Biorefinery concept, using renewable biomass feedstock for producing biofuels and
chemicals. Such conversions are aimed at producing the high-value products which enhance
profitability and in some cases, offer an incentive for fuel production. Biorefining is still largely
unexplored territory and presents unique challenges as the bioderived molecules invariably contain
more than one oxygen atom. This basic difference from the fossil derived hydrocarbons, demands
design of appropriate catalysts with mostly multifunctional sites for efficiently carrying out the
cascade type reactions in a single pot. Another interesting feature of bio-derived substrates is that
these are multi product reactions (MPR). Hence integration of catalyst design with the optimization of
process conditions makes it possible to achieve the desired product distribution. Among various bio-
feedstock options, co-generated glycerol in biodiesel production and abundantly available
lignocellulosic material at lower cost can be easily converted to a variety of starting materials.

This talk will cover highlights of our recent work on heterogeneous catalysts development for (i) bio-
glycerol hydrogenolysis to C3/ C2 diols and propanol all of which are commercially important. (ii)
carbonylation of bio-glycerol with urea to give glycerol carbonate while the transesterification with
DMC to give another high value product, glycidol (iii) downstream processing of cellulose derived
levulinic acid (LA) to produce γ- valerolactone (GVL) (iv) furfural is also a versatile carbohydrate
derived starting material for either direct hydrogenation to give a variety of useful products such as
furfuryl alcohol (FAL), tetrahydrofurfuryl alcohol (THFAL), 2-methylfuran (2-MF) and 2-methyl
tetrahydrofuran (2-MTHF) or via catalytic alcoholysis (esters of LA) / hydrogenation sequence to give
GVL (v)self etherification and reductive cascade etherification of 5-(hydroxy methyl) furfural (5-
HMF) to cetane enhancers. All these products have extensive applications as green solvents, fuel
additives and as monomers for a variety of polymeric products. The underlying basic aspect of
structure-activity relation required for catalyst design will also be discussed.

References

1. C. V. Rode, et al. US Pat. No. 8,809,593 B2, 2014.

2. R. B. Mane, C. V. Rode, Green Chem. (2012) 14, 2780-2789.
3. A. M. Hengne, C. V. Rode, Green Chem. (2012) 14, 1064 – 1072.
4. A. M. Hengne, S. B. Kamble, C. V. Rode, Green Chem. (2013) 15, 2540 – 2547.
5. N. S. Biradar, A. M. Hengne, S. N. Birajdar, P. S. Niphadkar, P. N. Joshi, C. V. Rode
ACS Sust. Chem. & Eng. (2014) 2, 272−281.
6. R. B. Mane, S. Patil, M. Shirai, S. S. Rayalu, C. V. Rode, Appl. Catal. B: Environmental (2017) 204,
134-146.
7. N. S. Date, N. S. Biradar, R. C. Chikate, C. V. Rode,ChemistrySelect, (2017) 2, 24-32.
8. S. E. Kondawar, C. R. Patil, C. V. Rode,ACS Sustainable Chem. Eng. (2017) 5, 1763-1774.
9. S. E. Kondawar, C. V. Rode,Energy & Fuels, (2017) 31 (4), 4361- 4371.
10. S. H. Shinde, C. V. Rode, Green Chemistry, 2017, 19, 4804 – 4810.
11. S. H. Shinde, C. V. Rode, ChemSusChem (2017) 20, 4090-4101
12. N. S. Date, R. C. Chikate, H. S. Roh, C. V. Rode, Catalysis Today, (2017) 10.1016/j.cattod.2017.08.002
 Translating Research on endophytic fungi into pharmaceutical and food
Application
Sunil Kumar Deshmukh
TERI-Deakin Nano Biotechnology Centre, The Energy and Resources Institute, Darbari Seth
Block, IHC Complex, Lodhi Road, New Delhi 110 003, India
e-mail: [email protected]

Endophytic fungi are defined as fungi that live asymptomatically within the tissue of higher
plants. These fungi came to limelight after the discovery of Taxol and Taxane from an
endophytic fungi Taxomycesandreanae, of Pacific yew. Later on, a large number of bioactive
metabolites from endophytic fungi have been isolated from endophytic fungi from tropical
countries. Still, there is a great opportunity to discover unexplored fungi with industrial
potential. There is a need to discover these fungi from less explored ecosystems e.g. cold
desert, hot desert, Antartica, mangroves along with other sources like likens, bryophytes,
orchids. Some of the strategies of cultivation of these fungi to stimulate the production of
secondary metabolites under laboratory conditions are needed to explore the diversity of
bioactive compounds. These strategies include variations in media composition, pH,
temperature, aeration, or shape of culturing flask; biotic elicitation by co-culture of different
strains; abiotic elicitation by physical or chemical stresses; and epigenetic modulation by
chemical epigenetic modifiers. These fungi are also known to produce antioxidants, food
colors and enzymes. Some of the work done in pharmaceutical and food industries and its
aspect of translation of endophytic fungi research into industrial applications will be
discussed.
 Total Synthesis Driven Methodologies
C. V. Ramana
Division of Organic Chemistry
CSIR-National Chemical Laboratory,
Pune - 411008, India; [email protected]

The structural complexity and skeletal diversity of natural products have served as
inspirations to organic chemists for the discovery and design of new synthetic methods en
route to their chemical synthesis. Our group focuses on the development of new
methodologies that are specifically designed in the context a total synthesis of natural
products of biological relevance. In this presentation, we wish to provide a comprehensive
compilation of various novel transformations that have been developed in our group along
with some salient aspects of the accomplished total synthesis.

References

1. Integrastain B:More, A. A. and Ramana, C. V. Org. Lett.2016, 18, 1458; More, A. A.

Ramana, C. V. Org. Lett.2016, 18, 612.
2. Trigolute B: Reddy, B. N. and Ramana C. V Tetrahedron 2017, 73, 888; Reddy, B. N. and
Ramana, C. V. Org. Lett. 2016, 18, 6264.
3. Propolisbenzofuran B:Kona, C. N. and Ramana, C. V. Chem. Commun. 2014, 50, 2152;
Srinivas, K. and Ramana, C. V. Org. Lett.2017, 19, 6466.
 Advances in Systematics , Applications and Conservation of Fungi
Sanjay K. Singh
National Fungal Culture Collection of India (NFCCI) - A DST-National Facility
Biodiversity and PalaeobiologyicsaGroup, MACS' Agharkar Research Institute,
GG Agarkar Road, Pune 411004, Email: [email protected]

Fungi exhibits amazing diversity behave as both friends and foes. Many fungi are beneficial
to human, plants, animal and environmental health. In contrast many of them are harmful and
act as pathogen causing diseases. Identification and characterization of fungi is the
cornerstone of many applied disciplines. Review reveals the devastating effects of some fungi
which has changed the world. On the other hand it has been relized that fungal biodiversity in
general can play an important role in generating bio-economy by exploring genetic and
biochemical diversity captured in natural resources and maintains them in a pure state in
germplasm bank and their authentication is a very important and strategic requirement for
developing innovative biotechnology processes and products. The basic approaches used in
detecting organism mostly rely on microscopic, cultural and morphological traits, require
extensive time, labour and through classical taxonomy knowledge. In addition, subject matter
specialist practicing in fungal identification is required for delivering effective results. Due to
the limitations in conventional methods, and plasticity in many morphological traits of fungi,
new molecular techniques developed and introduced from time to time for the investigation
and rectification of identification and classification problems. A high level of molecular
methods is increasingly becoming valuable tools in all aspects of fungal diagnostics,
biodiversity analysis and various applications. Due to these advances global dimensions of
fungi have changed tremendously and have opened improved prospects for basic and applied
researches.

The current trends are towards exploring a wide diversity of fungal cultures for applied
research, and it is becoming increasingly difficult to define and delimit which groups of fungi
are important for technological developments. Fungi, as a whole being principal source of
bioactive metabolites have established their credentials over the years as promising
goldmines for a variety of bioactive metabolites and enzymes. Several economically
important fungal genera which impacts our lives are being re-investigated taxonomically and
systematically, like Aspergillus, Penicillium, Colletotrichum, Cercospora, etc. for better
understanding of their biodiversity, biology, and biotechnological applications.

Among genera being reinvestigated, Fusarium is another important one. They survive in most
soil; arctic, tropical, desert, cultivated and non-cultivated field. Due to their potent pathogenic
behaviour they make their worldwide presence and cause a range of diseases leading huge
losses. About 300 records of different species and forma specialis belonging to more than 40
different species of Fusarium reported from various hosts/substrates in India. About 150
isolates from diverse substrates and geographic locations in India were studied in detail at
NFCCI. A glimpse of the new generic/species concept and highlights of the status of research
and development of Fusarium and in India shall be discussed during conference.
 Saroglitazar - - A CMC (Chemistry,Manufacturing and Control)
Perspective
Dr.Bipin Pandey

Center of Excellence (NFDD), Chemistry Dept.,Saurashtra University, Rajkot

The CMC perspectives of First New Drug designed, discovered, developed and launched by
an Indian Pharma company, ZydusCadila, Ahmedabad, will be described. Saroglitazarwas
launched in Sept.2013 in India as Lipaglyn, for the treatment of diabetic dyslipidemia. Its
chemistry, synthesis, manufacturing, impurities, IP issues, polymorphs and a broad overview
of how impurities are formed, during development stage, will be discussed. The importance
of understanding acid, base, oxidation, reduction, organometallic, catalytic, thermal,
photochemical, stereochemical, dissolution and analytical aspects of API’s and Intermediates,
for predicting probable impurities, involving 8 reactive species of carbon and 5 reactive
species of nitrogen, will be discussed.
 Metabolic engineering facilitates developing designer bacteria for
improving human health and plant growth.
G. Naresh Kumar

Department of Biochemistry, Faculty of Science, M. S. University of Baroda

Vadodara – 390002. Email :[email protected]

Genetic engineering facilitated exploiting a few bacteria for producing antibiotics, vitamins,
many organic molecules and proteins (enzymes). However, expanding knowledge of
biochemical, molecular biology and genetic manipulation aspects of a variety of bacteria
enabled to design diverse bacteria for the benefit of human health and agriculture. Metabolic
disorders have been increasing at an alarming rate in humans due to a variety of nutritional
abnormalities and environmental toxicants. Probiotic bacteria are gaining prominent role in
ameliorating these problems. Our genetic and metabolic engineering approaches enabled to
transform probiotic bacteria to convert sugars into prebiotics, ameliorate the toxic effects of
carcinogens, heavy metals and arsenate in rat experiments. On the other hand, metabolic
engineering of rhizobacteriavizPseudomonas, Herbaspirillum and Enterobacter enabled
secretion of gluconic, 2-ketogluconic, oxalic and citric acids transforming them into effective
phosphate biofertilizers.
 Oral Presentation

Synthesis and Biological Evaluation of Diversely Substituted Chroman

Derivatives ViaUgi Reaction
Kaushikkumar S. Lunagariya and Ranjan C. Khunt*
Department of Chemistry, Saurashtra University, Rajkot-360005
*E-mail: [email protected]

Abstract: An efficient protocol for the synthesis of diversely substituted chroman derivatives
has been developed by multi component Ugi reaction. A catalytically free, simple and
covineant reaction conditions were established. In order to develop better reaction condition,
the reaction was carried out at different optimized conditions. The synthesized compounds
are well characterized by known spectroscopic technique and were subjected to antitubercular
screening.
Keyword: Chroman,Efficient protocol, Ugi reaction, Antitubercular screening.
 Oral Presentation

Elucidating the metabolic basis of cancer using yeast as a surrogate:

A model for tumorigenesis

Jaswandi U. Dandekar*, Abhay Kumar¶, PaikeJayadeva Bhat¥

*
Department of Microbiology, Marwadi University, Marwadi Education Foundation, Rajkot 360 003,
India
¶
Department of Transplant Immunology and Immunogenetics, All India Institute of Medical Sciences,
New Delhi 110 029, India
¥
Laboratory of Molecular Genetics, Department of Biosciences and Bioengineering, Indian Institute
of
Technology Bombay, Mumbai 400 076, India

Tumor cells distinguish from normal cells by fermenting glucose to lactate in

presence of sufficient oxygen and functional mitochondria, a phenomenon referred to as
Warburg effect. Crabtree effect was invoked to explain the biochemical basis of Warburg
effect by suggesting that excess glucose suppresses mitochondrial respiration. Ithas been
known for long that yeast Saccharomyces cerevisiae display Warburg effect and Crabtree
effect during growth on abundant glucose. Beyond this similarity, it was also demonstrated
that expression of human pro-apoptotic proteins like Bax and p53 in S. cerevisiaeleads to
apoptosis. Here, we demonstrate that p53 expression in S. cerevisiae (Crabtree positive yeast)
causes apoptosis and increase in ROS levels when cells are growing on non-fermentable
carbon source like glycerol but not on fermentable carbon source like sucrose, a feature
similar to tumor cells. In contrast, in Kluyveromyceslactis(Crabtree negative yeast) p53
causes apoptosis and increase in ROS levels regardless of the carbon source. Interestingly,
the increased ROS levels and apoptosis are correlated to increased oxygen uptake in both S.
cerevisiae and K. lactis. Based on these results, we suggest that at least in yeast, fermentation
per seis not a prerequisite for escape from apoptosis. Rather Crabtree effect plays a crucial
role in determining whether the cells should undergo apoptosis or not.
 Oral Presentation

A novel salt-tolerant rhizosphericBacillus safensisS8, improves growth of

pearl millet under saline condition
Kalpna D. Rakholiya*1, Satya P. Singh1, Mital J. Kaneria1, V. D. Vora2
1
Department of Biosciences (UGC-CAS), Saurashtra University, Rajkot – 360005, Gujarat
2
Main Dry Farming Research Station, Junagadh Agricultural University, Targhadia (Rajkot)-360003,
Gujarat, India

Email ID: [email protected], [email protected]

ABSTRACT

Aim: Development of an effective plant growth promoting rhizobacteria (PGPR) inoculant

necessitates a diverse set of traits that can help its colonization in the rhizosphere and survival
under varying environmental conditions. Methods: The PGP ability of the bacterial isolate
S8 was evaluating for biofertilisation (phosphate solubilization and ammonia production),
biostimulation [indole acetic acid (IAA) production] and bio-control (HCN production,
hydrolytic enzyme production and antagonistic effects) activities. The efficacy in augmenting
salt tolerance in pearl millet under NaCl stress (0mM, 100 mM, 200mM). Results: Isolate
S5from the rhizosphere of pearl millet grew at up to 15% NaCl (w/v) and displayed specific
PGPR traits, such as the production of IAA, siderophore, ammonia, HCN, P-solubilisation,
hydrolytic enzyme production and their bio-control efficiency. Characterization of this isolate
using polyphasic approaches involving both phenotypic and genotypic attributes led to its
identification and designation as Bacillus safensisS8. Conclusion:Bacillus safensisS8
appears as effective PGPR inoculants as it possesses a number of traits useful in
establishment and proliferation in saline regions. Further studies on its pot trail applications
are in progress.

Acknowledgments

The Authors are thankful to the DST- Science and Engineering Research Board (SERB),
New Delhi, India for providing financial support under National Postdoctoral Fellowship
(NPDF) scheme (File No. PDF/2015/000430/LS, 06 June, 2016).
 Oral Presentation

Biodegradation of Textile dye Effluent using Bioreactors – Tactics of

Immobilization of Laccases
Dr Aditee Pandya
HVHP Institute of Post Graduate Studies and Research
KadiSarvaVishwavidyalaya
[email protected]
Mobile: 9687657444

Rhizopusoryzae and a purified laccase from this organism were able to degrade
triarylmethane, indigoid, azo, and anthraquinonic dyes and textile dye effluent that contained
these dyes. Initial decolorization, degradation and detoxification velocities depended on the
substituents on the phenolic rings of the dyes. Immobilization of Rhizopusoryzae laccase on
Scotch Brite enhanced the thermal stabilities of the enzyme and its tolerance against some
enzyme inhibitors, such as halides, copper chelators, and dyeing additives. Treatment of
effluent with the immobilized laccase almost reduced their toxicities. Detoxification reaches
to almost 98% and there was undocked biodegradation and decolorization that would be
blossoming in environmental pollution. A new era towards Green Revolution.
 Oral Presentation

Analytical Method Development and Validation of Pharmaceutical

Products ---- A Triumph for Synthetic Drugs
Dr Chintan Pandya
Assistant Manager
Torrent Pharamaceuticals Limited
[email protected]
Mob: 9687657333
Gujarat

The development of sound Analytical method is of supreme importance during the process of
drug discovery, release to market and development, culminating in a marketing approval. The
main objective is to review the method development, optimize and validation of the method
for the drug product which is API from the developmental stage of the formulation to
commercial batch of the product. Method development for the interested component in
finished product or in process tests and the sample preparation of drug product and to provide
practical approaches for determining selectivity, specificity, limit of detection, limit of
quantitation, linearity, range accuracy, precision, recovery solution stability, ruggedness, and
robustness of liquid chromatographic methods by UPLC to support the Routine, in process
and stability analysis. The positive result would be the capstone of success.
 Oral Presentation

Production and Charcterization of Pigments Produced By

EpicoccumPurpurasense MTCC 9351
Adarsh Kumar Singha,b, Dr.Neeta Raj a,b
a)
Lovely professional university Jalndhar,Punjab
b)
School of Biotechnology, Jalndhar,Punjab

ABSTRACT
Colour is a vital constituent and is probably one of the first characteristics perceived by the
senses. In food industry various synthetic colours are used and these colour are very harmful
for human beings, so with the increasing awareness of toxicity of synthetic colours, demand
for pigments from natural sources has increased in now days. Natural coloursare generally
extracted from fruits, vegetables, roots and microorganisms and are often called “biocolours”
because of their biological origin. Various synthetic colouring agents have the potential of
carcinogenicity and teratogenicity. So many microorganisms like Monascuspurpureus,
Penicillium sp. ,Epicoccumetc can be explored to produce pigments in suitable conditions.
Keywords- Epicoccum, Biocolours, synthetic colours,pigments,microorganisms
 Oral Presentation
Development of Deuterium Labeled Pharmaceutically Active Compounds
Sabera Bijania , Anamik Shah*b
a
Assistant Professor, Department of Chemistry, Marwadi University, Rajkot – 363003.
b
Vice- Chancellor, Gujarat Vidyapith, Ahmedabad

Key Words: Mixed catalyst, Deuteration, Mesalamine, C-H activation, Deuterated drugs

Abstract: A convenient and efficient lab-scale protocol for stable deuteration of Mesalamine,
with mixed catalyst 10% Pt/C (25 wt%) and 10% Pd/C (10 wt%) at 145°C, using D2O as
deuterium source, in hydrogen atmosphere, is reported.The nature of reactive species with
Pd/C–Pt/C–D2O–H2 system issuggested to be of electrophilic nature D+type.

COOH
COOH
99.7 D OH
H OH [Pd/C+Pt/C]
D2O
0
H2N D
H2N H 145 C , H2 atms. 99.8
D
H 99.8
 Oral Presentation

Stimulation of the growth of Vignaradiata under saline condition by the

plant growth promoting bacterium Bacillus sp.M124
Sneha H. Vaishnav, Mital J. Kaneria, Kalpna D. Rakholiya*, Satya P. Singh,
1
Department of Biosciences (UGC-CAS), Saurashtra University, Rajkot – 360005, Gujarat

EmailID: [email protected], [email protected]*, [email protected]

ABSTRACT

Aim:Plant growth promoting rhizobacteria (PGPR) enhance the plant growth by direct and
indirect mechanisms and enhance the growth productivity of agricultural crop in saline
condition. Methods:Bacillus sp. M124 isolated from the rhizospheric soil of pearl millet
from Morbi district, Gujarat, India.This study was carried out to evaluate the efficacy of
isolate M124 for indol-3-acetic acid (IAA) production, phosphate solubilization, ammonia
production and secretion of hydrolytic enzyme. The isolate was then used as an inoculant for
the vegetative study of V. radiata plant with different treatment of NaCl concentration.
Results: Isolate M124from the rhizosphere of pearl millet grew at up to 15% NaCl (w/v) and
displayed studied hydrolytic enzyme production and showed varied level of IAA production
at different time interval. It also able to solubilize phosphate. The isolates also enhance the
growth of V. radiate in presence of saline condition. Conclusion: The results validate the
Bacillus sp. M124 could be use in production of plant growth promoting effect for
agricultural crops for development of eco-friendly sustainable agriculture.

Keywords:Bacillus sp., salt tolerant, Phyto-hormones, hydrolytic enzyme production,

ammonia production, seed germination, phosphate solubilization

Acknowledgments

The Authors are thankful to the DST- Science and Engineering Research Board (SERB),
New Delhi, India for providing financial support under National Postdoctoral Fellowship
(NPDF) scheme (File No. PDF/2015/000430/LS, 06 June, 2016).
 Multi-trait plant growth promoting (PGP) rhizospheric bacteria isolated
from medicinal plant Leucasalba

Dhrupa Mayatra2, Riddhi Chaniyara2, Kana Parmar2, Krupali Sureja2, Kalpna D.

Rakholiya*1, Mital J. Kaneria1, Satya P. Singh1,
1
Department of Biosciences (UGC-CAS), Saurashtra University, Rajkot – 360005, Gujarat
2
Instituteof Biotechnology, Department of Biosciences (UGC-CAS), Saurashtra
University, Rajkot – 360005, Gujarat
Email ID: [email protected], [email protected],

Abstract

Aim: in recent years, pathogenic attacks are one of the major threats to the growth and
productivity of crop plants. Currently, instead of use of synthetic fungicides, the plant growth
promoting bacteria has been considered eco-friendly in nature. Against, soil saline
environment root associated beneficial bacteria can help improve plant growth and nutrition.
Methods: four salt tolerant PGPR strains were isolated from rhizosphere of Leucas alba
from saurashtra university, Rajkot, Gujarat, India. All the PGPR strains were able to show
growth at up 5% NaCl (w/v). The isolation was done in four different media (NA, KB,
Jenson’s Media, ASM agar). Phosphate solubilization, ammonia, and IAA secretion of
rhizospheric strain was tested. Moreover, bio-control (hydrolytic enzyme production and
antagonistic effects) activity also measured. Results: SULA 7 showed highest percentage
inhibition against Rhizoctoniasp. All isolates showed varied level of IAA, ammonia
production at different time intervals. Conclusions: PGPR strains isolated under present
investigation may be useful as a novel biofertilizers for crop production at saline region.
Further studies on its biochemical and molecular identification are in progress.

Keywords: Rhizospheric bacteria; Antifungal production; Agricultural applications, IAA

Acknowledgments

The Authors are thankful to the DST- Science and Engineering Research Board (SERB),
New Delhi, India for providing financial support under National Postdoctoral Fellowship
(NPDF) scheme (File No. PDF/2015/000430/LS, 06 June, 2016) as well as Prof. RK Kothari,
Head & Co-ordinator of Institute of Biotechnology for providing excellent research
laboratory facility.
 COMPARATIVE ASSESSMENT OF ANTIOXIDANT ACTIVITY AND
PHYTOCHEMICAL ANALYSIS OF TWO PLANTS PEELS BELONGS
TO RUTACEAE FAMILY USING DIFFERENT EXTRACTION
TECHNIQUES

PavanBharai, SurbhiParmar, MahipalRathod, KalpnaRakholiya, MitalKaneria*, Sumitra

Chanda

Phytochemical, Pharmacological and Microbiological Laboratory,

Department of Biosciences, Saurashtra University, Rajkot-360 005, Gujarat, India
*E-mail: [email protected]

Abstract
This study was designed to evaluate the antioxidant activity of two plants peels of Rutaceae
family. The extraction was done by individual cold percolation (Petroleum ether, acetone,
methanol, aqueous), Infusion, maceration (methanolic&ethanolic), decoction, ultrasonication
and microwave assistant extraction methods. The antioxidant activity was evaluated using
antioxidant assay, 2, 2-diphenyl-1-picryl hydrazyl free radical scavenging assay. Total phenol
and flavonoid content was also measured. The antioxidant activities showed different levels
in different extracts. This suggests that significantly influences the choice of solvent and
methods for extraction. This study demonstrated that peels of both plants, could serve as good
source of antioxidants for use in the preparation of dietary supplements or nutraceuticals,
food ingredients, pharmaceutical, and cosmetic products.
 The life change is possible without altering DNA
Mutva Amir M *, Patel Bharat K*, Khatri Dinesh K, KhokharSafina S, Patel Nipa H
and Patel Mahek D.

Smt .S.S.PatelNootan science & commerce college, visnagar-384315

Abstract
Revolution of life through the belief. The implications of this research radically
change our understanding of life. It shows that not only genes and DNA control our biology;
that instead DNA is controlled by signals from outside the cell, including the energetic
messages emanating from our positive and negative thoughts. In this era quantum biology is
being hailed as a major breakthrough showing that our bodies can be changed as we retrain
our thinking.

While the eukaryotic genome is the same throughout all somatic cells in multicellular
organism, there are specific structures and functions that discern one type of cell from
another. These differences are due to differential gene regulation during developmental stage
as well as healthy and diseases condition. Interestingly, these cell-specific gene expression
patterns can be affected by an organism's environment throughout its lifetime leading to
phenotypical changes that have the potential of altering risk of some diseases. Both cell-
specific gene expression signatures and environment mediated changes in expression patterns
can be explained by a complex network of modifications to the DNA, histone proteins and
degree of DNA packaging called epigenetic marks. Several areas of research have formed to
study these epigenetic modifications, including DNA methylation, histone modifications,
chromatin remodeling and microRNA (miRNA).

Keywords: The belief, control internal environment through positivity, Epigenetics, gene
expression pattern change by mi RNA as well as modification of histone and DNA.
 A convenient and facile Synthesis of Coumarino Imidazole derivative
- An approach towards Green Chemistry
AbhayBavishi,* Yvonne Fernandes, SushmitaGangunly and ShaileshThakrar

Department of chemistry,
Christ College, Rajkot
*E-mail: [email protected]

In present world process chemistry has a noteworthy importance. To improve

pathway by undergoing less steps, and less consumption of energy and solvent free reactions
by carrying out various trials. Coumarin and imidazole moiety being of vital pharmacological
importance, the present work is related to fuse the imidazole ring at 3,4 position of the
coumarin. Work includes a facile and convenient and solvent free reductive cyclization of
imidazole ring on the coumarin ring. The aim of the studies was to develop a product by
different pathway and high yield. The entire synthesized compounds were confirmed
different spectroscopic techniques such as NMR, Mass, IR and Elemental analysis
 ISOLATION AND SCREENING OF LACTIC ACID PRODUCING BACTERIA FOR
BIOTECHNOLOGICAL PURPOSE

Payal chahodiya, Darshan marjadi

Shree ramkrishna institute of computer education and applied sciences .surat-gujarat

ABSTRACT

Lactic acid bacteria is group of gram positive organism which have the property of converting lactose
and other sugars to lactic acid through fermentation of carbohydrates. Lactic acid bacteria produce
organic acid mainly lactic acid which have ability to inhibit the growth of many especially pathogenic
gram negative bacteria, so whey water the translucent liquid rich in lactose, vitamin, protein obtain as
by product after precipitation of curd used as the starter medium for lactic acid bacteria for lactic acid
production.

The main aim of this work was to study the fermentation of whey for the production of lactic acid.
The effect of different process parameters such as temperature, inoculums size, incubation time and
pH of the medium is carry out to check the conversion of whey sugar to lactic acid.

x
 Synthesis and antimicrobial evaluation of some new 1,3,4- oxadiazoles
Vishal B. Mulani, Purvesh B. Dobariya, Dinesh R. Godhani*
Department of Chemistry (UGC NON-SAP & DST-FIST sponsored), Mahatma Gandhi Campus, Maharaja
Krishnakumarsinhji Bhavnagar University, Bhavnagar-364002, Gujarat, India
E-mail: [email protected]

ABSTRACT:
Recently the investigations in the field of oxadiazole have intensified due to the large number of uses of
oxadiazoles in the most diverse areas, 1,3,4- oxadiazole derivatives have been reported to show biological
activities like bactericideand fungicideproperties. These observations and our previous workof oxadiazole
prompted us to synthesize unreported derivatives of 1,3,4- oxadiazole. A series of 2-((4-acetyl-5-(aryl)-5-
methyl-4,5-dihydro-1,3,4-oxadiazol-2-yl)methylthio)-3-o-tolylquinazolin-4(3H)-one was synthesized by the
cyclization of imines using acetic anhydride. The Schiff base are obtained by the reaction of appropriate
carbonyl compound with 2-(4-oxo-3-o-tolyl-3,4-dihydroquinazolin-2-ylthio) acetohydrazide. The structure of
synthesized compounds was characterized by IR, 1H-NMR, 13C-NMR and mass spectrometry. The synthesized
compounds were screened for their antimicrobial activity against different strains of Gram-negative (E. coli and
P. aeruginosa) and Gram-positive (S. aureus and S. pyogenus) bacteria and selected fungi C. albicans, A.
nigerand A. clavatus using serial broth dilution method. Our approach is to focus on the modification of
synthetic pathway for the said reaction with respect to time and other physico-chemical parameters.
 “Stem Cells” – A Therapeutic Boon , No Science Fiction Anymore
ShivaniJani ¹,Nimesh V. Rupala ¹, Tauka Mehta ², Priya Mehta ³*

¹ Shree M & N Virani Science College, Rajkot - 360005, Gujarat, India.

² L J Institute of Life Sciences, Ahmedabad – 382210, Gujarat, India.

³ C U Shah Institute of Life Sciences, Surendranagar – 363030, Gujarat, India.

*Corresponding author : [email protected]

Stem cells are an unspecialized cells having the capacity for self-renewal and capability of
proliferation and differentiation to various cell lineages. Stem cells have the remarkable
potential to develop into many different cell types in the body during early life and growth. In
addition, in many tissues they serve as a sort of internal repair system, dividing essentially
without limit to replenish other cells as long as the person or animal is still alive. They are
vital to the development, growth, maintenance, and repair of our brains, bones, muscles,
nerves, blood, skin, and other organs. They can be classified into embryonic stem cells (ESC)
and non-embryonic stem cells (non-ESC). Regenerative medicine, the most recent and
emerging branch of medical science, deals with functional recovery of tissues or organs for
the patient suffering from severe injuries or chronic disease. The spectacular progress in the
field of stem cell research has laid the foundation for cell based therapies of disease which
cannot be cured by conventional medicines. Advancements in gene editing and tissue
engineering technology have endorsed the ex vivo remodelling of stem cells grown into 3D
organoids and tissue structures for personalized applications. This Brief review elucidate the
tremendous potential of stem cells in Therapeutics and Clinical Medicine.

Key Words: Stem cells, Regenerative medicine, Therapeutics, Therapy.

 Citric acid production from pineapple waste by Aspergillus niger
Khushbu Patel&Darshan Marjadi
Shree Ramkrishna Institute of Computer Education and Applied
Sciences,Surat,Gujarat,India.
Abstract
A Submerged fermentation used for citric acid productionfrom pineapple waste by
Aspergillus niger. The media was supplemented with glucose, sucrose, ammonium nitrate,
ammonium phosphate,coppersulphate and clacium chloride with optimum pH. It was found
that pineapple waste with sucrose and ammonium nitrate gave the optimum citric acid when
fermented for 5 days at optimum temprature with optimum moisture content.Theyeild was
based on the amount of fermentable sugerconsumed.The results present the use of pineapple
waste as a cheap medium for the production of citric acid by Aspergillus niger.
 Potential application of Bacillus subtilis lipopeptides in
toothpaste formulation.
By ,Shraddha Mandaviya , Darshan Marjadi

Department of Biotechnology ,Shree Ramkrishna Institute of Computer

Education & Applied Sciences.Surat, Gujarat ,India.

ABSTRACT

Biotoothpaste is the toothpaste that contains biologically active ingredient. Toothpaste

contains sodium lauryl sulfate (sls) as an anionic surfactant, emulsifier and cleaning agent. In
the present work Bacillus subtilis was used as a source for the production of bio surfactant
(lipopeptides) or emulsifiers. After 2 days of production period bio surfactant was extracted
using acid alkali precipitation method. And finally obtained powdered bio surfactant was
used along with the other ingredients for the formation of bio toothpaste. The
physicochemical properties were analyzed considering several tests mainly spreading ability,
water activity, pH, foaming and cleaning tests. The obtained results indicated that the bio
surfactant was as efficient as the chemical surfactant confirming its potential utilization in
toothpaste formulation compared to the commercial one. The evaluation of the antimicrobial
activity was detected. The results showed that the biotoothpaste exhibited an important
antimicrobial activity.
 Defective Green Coffee Beans as Nutrient Source for Pesticide Degrading
Bacteria
Patel Foram and Marjadi Darshan
Department of Biotechnology, Shree Ramakrishna Institute of Computer Education and Applied
Sciences, Surat, Gujarat, India
E-mail : [email protected]

Abstract

Generally glucose, peptone, meat and beef extract used as primary substrates in the study of
pollutant cometabolism. In the presence of more favorable carbon sources can inhibit the
degradation of xenobiotics so sometimes primary substrates fails. To overcome this problem,
natural wastes maybe used. Defective green coffee brand may be great source as primary
substrate. Green coffee beans has a great chemical and biological complexity, and it used as
co-substrate to remove toxic recalcitrant pollutants. From this defective green coffee beans,
four bacteria strains were isolated. This four bacterial strains are capable to grow and remove
DDT [1,1,1-trichloro-2,2-bis (4-chlorophenyl) ethane] and PNCB [ 1-CHLORO-4-
NITROBENZENE] in a liquid medium. Result showed that defective green coffee beans was
an ample nutrient source for bacterial growth and it significantly enhanced DDT and PNCB
biodegradation in comparison with glucose.
 Isolation and screening of Polyhydroxyalkanoates producing halophilic
bacteria from mangrove soli sample
Viradiya Dhruval and Marjadi Darshan
Department of Biotechnology, Shree Ramakrishna Institute of Computer Education and
Applied Sciences, Surat, Gujarat, India
Email ID ⦂ [email protected]

• Abstract⦂⦂

Polyhydroxyalkanoates (PHAs) are storage materials that accumulate by various bacteria as

energy and carbon reserve materials. They are biodegradable, environmentally friendly, and
biocompatible bioplastics. Unlike petrochemical-based plastics that take several decades to
fully degrade, PHAs can be completely degraded within a year by variety of microorganisms
into CO2 and water. In this study, I isolate mangrove soil sample from konkan coast, Arabian
sea (dumas beach) Were collected for the isolation of microorganism. Which are responsible
to production of PHA. Those strain are inoculated in to E2 mineral medium for several days
at 37°c with rotary shaker at 180 rpm, after 30 h withdraw sample for cell dry weight(CDW)
and PHA content analysis, and we can also check the effect of NaCL concentration, PH, and
nitrogen source on growth of PHA producing bacteria.
The objective of the present work is to isolate halophilic bacteria from mangrove soil
samples and screen the bacterial isolates for their ability to utilize carbon source to produce
PHA.
Role of Chitosan in Encapsulation of Nanofertilizer to Enhance Production
in Agriculture
NageshGawade*, Prabhakar Kore, Suhail Ahmad and AtulDhansil
Junagadh Agricultural University, Junagadh, Gujarat

[email protected]

Abstract
Nanotechnology is the the art and science of building stuff that does stuff at the
nanometer scale. Nanotechnology (sometimes shortened to "nanotech") is the study of
manipulating matter on an atomic and molecular scale. Generally, nanotechnology deals with
structures and sized between 1 to 100 nanometers in at least one dimension, and involves
developing materials or devices within that size.
Nowadays nanofertilizers are taking special attention in agriculture research for better
growth and productivity. Nanoferlizers are the fertilizers works at nanoscale synthesized
using nanotechnology. They are important tools in agriculture to improve crop growth, yield
and quality parameters with increase nutrient use efficiency, reduce wastage of fertilizers and
cost of cultivation. Nanofertilizers provide more surface area for different metabolic reactions
in the plant which increase rate of photosynthesis and produce more dry matter and yield of
the crop.
Chitosan is a biopolymer, a chitin derivative, a compound which is completely safe
for the environment. Due to its polymeric cationic, biodegradable, bioabsorbable and
bactericidal characteristics, chitosan (CS) nanoparticle is an interesting material for use in
controlled release systems. Chitosan is obtained as a result of chemical or enzymatic chitin
deacetylation
The encapsulated fertilizers, in which fertilizers are entrapped within nanoparticles
and protect it for better survival in inoculated soils, allowing for their controlled release into
the soil. The method of encapsulation of fertilizers components in polymeric, chitosan
nanoparticle is relatively novel with potential commercial applications. Accelerating plant
growth and productivity through the application of nanofertilizers can open new perspectives
in agricultural practices, because nanofertilizers promise to be a safe way to enrich nutrients
to plants without doing harm to the environment.
 EFFECT OF CHLORPYRIPHOS DEGRADATION BY
JR16NUTRITIONAL AND ENVIRONMENTAL PARAMETERS ON
KinjalDholakiya, MamtaChudasama, Jalpa Rank,Ramesh K. Kothari*

UGC-CAS Department of Biosciences, Saurashtra University, Rajkot- 360005, Gujarat, India

Abstract:

Chlorpyriphos is a member of the organophosphate class of insecticides. This class has

become one of the most widely used groups of pest control chemicals. In 1989 nearly 40%
of the $6.2 billion global insecticide market was comprised of organophosphates (OPs).
Chlorpyriphos is registered for use in nearly 100 countries and is annualy applied to approx
8.5 millions crop acres. CPP is used to kill number of pests including insects and worms.
Effect of several nutritional and environmental parameters was checked on chlorpyriphos
degradation by JR16. The optimum conditions were observed to be 20 h old inoculum, 5%
inoculum size, static culture conditions, 28◦C temperature and pH 7.0. The maximum
growth was observed in sucrose as carbon source and yeast extract as nitrogen source in
chlorpyriphos containing Bushnell Hass medium.

Keyword: Organophosphate, Chlorpyriphos, Optimization, Degradation

*Correspondence:
Ramesh K. Kothari
Professor,
Department of Biosciences, Saurashtra University, Rajkot – 360 005, Gujarat, INDIA
[email protected]
Phone No. +91 94285 98941
 Effect of ACC-deaminase producing Bacillus cereus on the growth of
Vignaradiata (Mung beans) under salinity stress
Vishal Kothari1, Jasminkumar Kheni1, B.R.M. Vyas2

Department of Biotechnology, JAU, Junagadh1

Department of Bioscience, Saurashtra University, Rajkot2

Abstract :
Bacillus cereus isolated from the rhizosphere of Brassica nigra growing in the saline desert
of Radhanpur (India), was identified on the basis of biochemical and 16S rDNA analysis.
Salinity stress induces higher levels of ethylene in plants which limits crop production. This
increased concentration of ethylene can be reduced by using plant growth promoting
rhizobacteria (PGPR) producing ACC-deaminase. Bacillus cereus produces ACC deaminase
(0.22 U.ml-1), siderophore (85% U), IAA (3.36 µg.ml-1) and solubilizes phosphate (150
µg.ml-1). B. cereus has the ability to grow over pH 5-11 and in the presence of up to15%
NaCl. Talc-based B. cereus formulation (2×10 8 cfu.g-1) was prepared and evaluated for its
plant growth promoting activity. Root elongation of Vignaradiata in salt stress conditions
(1.2 S.m-1) was 3.6 cm while in control it was 2.5 cm. The results show that salinity stress
decreased mung bean growth significantly but inoculation of B. cereus reduced the inhibitory
influence of salt stress on mung bean growth.
 Histological studies of Leaf Regenerated Cultures of Biodiesel Crop
(Jatropha curcas L.)
Jasminkumar Kheni1, Vishal Kothari1, J.Chikara2

Department of Biotechnology, JAU, Junagadh1

CSMCRI, Bhavnagar2
[email protected]

Abstract:
Jatropha curcashas attracted the attention of scientists and entrepreneurs equally as a natural
source of biodiesel. The plant being wild in nature, has erratic behaviour in seed yield
production. Therefore, few elite plants were selected on the basis of consistant yield
behaviour and oil content for mass propagation through tissue culture. Attempts were also
made to regenerate the plants through direct organogenesis. Here we reports histology of
leaf regenerated cultures showing direct organogenesis rather than callus formation.
Histological sections (6µM) prepared during culture initiations suggest that leaf as
explants can be used for direct organ formation so as to reduce the time period taken for
generating the plantlets indirectly via Callus formation. We also did comparative studies of In
vitro and In vivo cultures of J.curcas through scanning electron microscopy (SEM). Major
differences were observed in midrib hairy structure and leaf stomata.
 Topic: Isolation and Screening of Cellulase Producing Bacteria using Fruit Peels

Name: Gargi Vijaybhai Manani

Class: M.Sc.(microbiology)

Department: Biosciences, Saurashtra University, Rajkot.

Mail ID: [email protected]

Abstract:

The present work has been undertaken for the isolation of cellulose producing bacteria and to
detect unit activity of cellulase by using fruit peel as a substrate. Cellulase producing
microorganism are most important in textile and paper industries. Soil sample from farmland
were used for the isolation of cellulase producing bacteria. Bacterial colonies were screened
for cellulase production on Carboxy Methyl Cellulose agar plate and zone of CMC utilization
was detected using iodine solution. The unit enzyme activity was measured by DNSA
method. Remarkable production of cellulase was achieved by 2.5% pineapple peel at 37⁰C
temperature.
 Isolation and Screening of Cellulase producing Bacteria using Fruit peels
Name: Sureja Amee

Class: M.Sc. (Microbiology)

Department: Biosciences, Saurashtra University – Rajkot

Mail Id: [email protected]

Abstract

Aim of present investigation was to isolate the Cellulase producing Bacteria and to detect the unit
activity of Cellulase by using fruit peels as substrate. Cellulase producing Microorganisms are most
important in industries with large application in textile industries and paper industries. Soil samples
from farm land were used for isolation of cellulase producing bacteria. Bacterial colonies were
screened for cellulase production on the CMC agar plate & zone of CMC utilization was detected by
using iodine solution. The unit enzyme activity was measured by DNSA method. Remarkable
production of Cellulase was achieved by 2.5% pineapple fruit peels at 37ᵒC temperature.

Key Words:Cellulase, Fruit peels, DNSA.

 Assessment of medicinal phytochemical extracts for their Quorum
inhibitory potential against Pseudomonas aeruginosa and
Erwiniacarotovora

Mehta Gunjankumar1*, Jadeja Vasantba2, Jadeja Pravina3

1
Department of Biotechnology, Shree M. & N. Virani Science College,
Rajkot- 360005, Gujarat, India
2
Department of Microbiology, Shree M. & N. Virani Science College,
Rajkot- 360005, Gujarat, India
3
Smt. Satguna C. U. Shah Home Sci., arts & Commerce Mahila college,
Wadhvan-363020, Gujarat, India
*Corresponding author: Mehta Gunjankumar, Email: [email protected]

Quorum sensing(QS) is a density dependent bacterial cell–cell communication process that

involves the production, detection, and response to extracellular signaling molecules known
as autoinducers. QS systems are ubiquitous in bacteria, and have since been found to regulate
diverse cellular functions including luminescence, biofilm formation, antibiotic production,
virulence factor expression, pigment production, plant-microbe interactions, mating and
motility. Pseudomonas aeruginosa is a nosocomial pathogen responsible for fatal pulmonary
infections, urinary tract infections and surgical site infections in immunocompromised
individuals. Erwiniacaratovoracauses soft rot and blackleg in potato tubers which leads to
great loss to agricultural commodities. Pathogenic attributes and virulence factors of these
pathogens are under control of QS. The compounds that inhibit cell-to-cell communication in
prokaryotes, known as Quorum sensing inhibitors(QSIs) has offered a novel method of
pathogen management in animals and plants. QSIs have been reported from algae and plant.
However, Indian medicinal plants have not been explored much. The present study explores
the potential of Indian medicinal plants as a source for promising QSIs against pathogenic
bacteria.

Keywords: Quorum sensing, Autoinducers, Phytochemistry, Extraction, Pathogenesis

 ONE-POT SEQUENTIAL APPROACH FOR THE CONSTRUCTION OF HIGHLY
FUNCTIONALIZED TRIAZOLO[4,3-c]PYRIMIDINES.

Dhananjay Pandya, Ashok Rathod, MayurShiyal, Prof. Y. T. Naliapara*

Department of Chemistry, Saurashtra University, Rajkot-360005 (Gujarat-India).

Email:[email protected]

Abstract:

Novel 1,2,4-triazolo[4,3-c]pyrimidine-8-carboxamides were synthesized via oxidative

cyclization of hydrazono-1,6-dihydropyrimidine-5-carboxamide intermediates by the
application of iodobenzenediacetate as a sole cyclizing agent. Here, we report a one-pot
sequential strategy to generate the corresponding triazolopyrimidines by condensation of
prepreparedacylketenedithioacetals and arylamidines. Moreover, this process describes the
application of presynthesizedarylamidines, which omits the Suzuki-Miyaura cross-coupling
reaction and hence provides metal-free organic synthesis in an atom and step economical
fashion.
Synthesis and antitumor activity of highly functionalized indole derivatives
Kishankumar C. Parsonda, Vivek R. Mandanka, Naval P. Kapuriya, Satishkumar D. Tala*

Department of Chemistry, Shree M. & N. Virani Science College (Autonomous),

YogidhamGurukul, Kalawad Road, Rajkot-360005 (Gujarat) India.

Abstract

We have successfully applied bioisoster approach for the design and synthesis of new
anticancer molecules from β-carboline motif. The newly synthesized molecules were tested
for their in vitro anticancer activity against various cancer cell growths. The most active
compounds from the newly synthesized derivatives were tested for their in vivo as well as
primary mechanistic study. We found that, these derivatives exhibits potent antitumor activity
against CCRF-CEM, PC3, H1299 & OECM1 solid tumour growths. The most potent
derivatives were further screened for in vivo study using xenograft model. Primary
mechanistic study revealed that they exhibit anticancer effect through DNA cross linking &
Topoisomerase inhibition.
 Synthesis and anticancer activity of nitrogen mustard derivatives
Milan B. Gadher, Tejas H. Padia, Anilkumar S. Patel, Pankajkumar B. Nariya*

Department of Chemistry, Shree M. & N. Virani Science College (Autonomous),

YogidhamGurukul, Kalawad Road, Rajkot-360005 (Gujarat) India.

Abstract

In the current project, we have synthesized a series of new water soluble N-mustard-benzene
conjugates (I, Fig. 1) prepared by linking phenyl N-mustard pharmacophore with benzene
moiety through a urea linker. This series of compounds were prepared via structure
modifications of Compound-A, previously synthesized in our laboratory, by bioisostere
approach. The benzene ring bears a variety of ω-N,N-dialkylaminoalkylamide or ω-
cyclicaminoalkyl amide side-chains located to the meta- or para-position of the urea linker.
The tertiary amino function on the side-chain can be converted into a variety of water-soluble
salts with various acids. The newly synthesized derivatives were subjected to evaluate for
their antitumor activities both in vitro and in tumor xenograft model. The results showed that
the newly synthesized conjugates were also found to have a broad spectrum of antitumor
activity against a panel of human leukemia and solid tumor cell growth in culture. Among
these derivatives, compound Compound-9b and Compound-9a were selected for further
antitumor studies. It was revealed the Compound-9b is more cytotoxic than Compound-Ain
inhibiting cell growth of various tumor cell growth in vitro. It also showed that this agent is
more potent than Compound-A against human colon HCT-116, prostate PC3, and lung
cancer H460 xenografts in mice with less toxicity. Studies on the mechanism of action
revealed that Compound-9b is able to induce DNA cross-linking and cell arrest at G2/M
phase. The present investigations conclude that Compound-9b has high potential to be
selected as a candidate for preclinical antitumor studies.
 A validated stability indicating chromatographic method for the
simultaneous estimation of Camylofin with NSAID drugs and a new
approach of method transfer from classical HPLC to a modern UPLC
instrument
Sheetal Makwana1, 2, Madhavi Patel1, Ankita dodiya1, Jatin Upadhyay2 and Anamik Shah1*
1
Center of Excellence in Drug Discovery, NFDD Complex, Department of Chemistry, Saurashtra
University, Rajkot-360005, Gujarat, India.
2
Matushri VirbaimaMahila Science & Home Science College, Rajkot.

ABSTRACT

The presented work describes the method development of simultaneous determination of

Camylofindihydrochloride (CMF), Diclofenac potassium (DCF) and Paracetamol (PCM)
using reversed phase high performance liquid chromatography (HPLC- UV) and the method
was further transfer to a new generation instrument; ultra performance liquid chromatography
(UPLC- PDA).The detailed validation carried out for the combination tablet formulation of
CMF and DCF by UPLC- PDA. From the method development study, Acquity UPLC HSS
C18 (2.1×50mm, 1.8µm) was finally selected for validation. The satisfactory results
observed for peak shape, retention time and resolution with a mobile phase of 20mM
ammonium acetate buffer (pH 3.0 with dilute ortho phosphoric acid): methanol (33:67v/v).
The elution of mobile phase was maintained at a flow rate of 0.250ml/min; isocratically and
detection was carried out at 220nm. Both of drugs were efficiently separated out in less than
3.5min with 1.1 and 3.2 min of retention time of the CMF and DCF with 11.87 of resolution.
The linearity was obtained in the 20.0-80.0µg/ml range of concentration with 0.9998 of
correlation coefficients for the substances. The method was analyzed for specificity; with
detailed force degradation study; which is a simple, precise and accurate method, as per the
International Conference on Harmonization (ICH) guidelines.
 Production of amylase using Banana waste by Bacilius subtilis
By, Madhavi Nimavat, Darshan Marjadi

Department of Biotechnology,

Shree Ramkrishna Institute of computer

Education & Applied sciences.

Surat, Gujrat, India.

ABSTRACT:

Amylase is one of the most important and of great significance . Amylase could
be potentially useful in the pharmaceutical, fine chemical industries of enzymes, medicinal
and analytical chemistry and other application. Amylase can be derived from several sources
,such as plants, animals and microorganisms. Banana waste was used as a substrate for the
production of amylase by Bacillus subtilis using solid state fermentation. First Bacillus
Subtilis was grown on nutrient broth. Then, this active culture was used as inoculum in the
production medium of amylase. Then substrate Banana peel was added to the medium . After
24 hours Amylase was extracted and Bioassay of amylase was performed. The various
parameter were optimized the incubation period, substrate concentration, pH and incubation
temprature.
 Microwave Assisted Cu(I)-CatalyzedHighly Efficient Approach for One-Pot Synthesis
of Pyrazole Derivatives Using A3 Coupling.
1,2
Kaushik D. Pambhar, 1,2Bharat Baraiya, 1,2Ranjan C. Khunt*, 1,2Anamik Shah*
1
Department of Chemistry, Saurashtra University, Rajkot, India.
2
Centre of Excellence, NFDD complex, Saurashtra University, Rajkot, India.

Email: [email protected]
Abstract:

CuBr-catalyzed three component one-pot A3 coupling reactions were investigated under

microwave irradiation.Although metal-catalyzed A3-coupling reactions have been
extensively used to synthesize various propargylamine. Till A3 coupling is not tested in many
heterocycles like substituted pyrazole.Pyrazole-4-carboxaldehydes, alkynes and amines with
a variety of structures have been tested against Copper based catalyst. Best results achieved
by Copper(I)bromide catalyst via microwave irradiation. Overall 15 subtracts of Pyrazole
based propargylamine was synthesize . A catalyst loading of 20 mol% was sufficient to give
excellent yields under microwave irradiation. In this study, set of reactions carried out under
various Cu (I) and Cu (II) catalysts as well as different solvents and different stoichiometric
ratio. This synthesis route made a great difference and resultant protocol was very
convenient and excellent yielding for the generation of a broad substrateof heterocyclic
substituted propargylamine.
Graphical Abstract:

Keywords:Pyrazole-4-carboxaldehydes, A3 coupling, Copper Catalyzed, Microwave

Assisted
Potassium tert-Butoxide Catalyzed Three Component Domino Reaction Strategy:
Synthesis of Triazolo[5,1-b]quinazoline and Benzimidazo[2,1-b]quinazoline Derivatives.

1,2
Ashish P. Dhamsaniya,1,2Denish Viradiya,1,2Rajesh kakadiya,1,2Shahrukhkhan Safi
,1,2Anamik Shah*
1
Department of Chemistry, Saurashtra University, Rajkot-360005, India.

2
Centre of Excellence (CoE), National Facility for Drug Discovery (NFDD) Saurashtra
University, Rajkot-360005, India.

Email:[email protected]

Abstract: Three-component reactions of α–tetralone with 1,2,4-triazol-5-amine/2-

aminobenzimidazole and aromatic aldehydes have been discovered by using potassium tert-
butoxide (t-BuOK) as a catalyst. A series of new and polyfunctionalized triazolo[5,1-
b]quinazolines and benzimidazo[2,1-b] quinazolines were synthesized. The significant
advantages of the developed strategy involve the construction of the corresponding
heterocycles by eliminating the use of precious catalysts under a mild condition in good
yields.

Graphical Abstract:

Keywords:2-Aminobenzimidazole, Benzimidazo[2,1-b]quinazoline, Domino reaction,

Potassium tert-butoxide, α–Tetralone, 1,2,4-Triazol-5-amine, Triazolo[5,1-b]quinazoline.
 “Multi component approach toward pyrazolo[1,5-a]pyrimidine; Design, synthesis and
characteristics studies”

Prakash L. Kalavadiya1 and Hitendra S. Joshi2*

Chemical research laboratory,Department of chemistry,Saurashtra university-Rajkot, 360005
E-mail: [email protected]

Abstract:
Nitrogen-containing heterocyclic compound great interest since they exhibit
numerous biological activities. In present work, we have synthesisindole-basedpyrazolo[1,5-
a]pyrimidin derivative viathree component one port reaction of 5-(1H-indol-3-yl)-1H-
pyrazol-3-aminewith malononitrile and various aromatic aldehyde. The significant advantage
of the developed strategy involves mild basic, environmentally friendly condition and having
a good yield at room temperature.

All the synthesized compounds are characterized by using various spectroscopic

techniques like 1H-NMR, 13C-NMR, Mass and IR spectroscopy.

H
R N

HN N
HN O TEA N
NH2 N N N
EtOH, RT
N H2N
R

Keyword: pyrazolo[1,5-a]pyrimidin, three component one port condensation,mild basic

condition, room temperature, domino reaction.

Reference:

1. A. El-Mekabaty, H. A. Etman, A. Mosbah. J. Heterocyclic Chem., 2016, 53, 89.

2. Johnny Slätt, Ivan Romero, Jan Bergman, synthesis, 2004, 16, 2760-2765.
3. Israr Ahmad, Neeraj Mishra, Tamal Ghosh, J Incl Phenom MacrocyclChem, 2013, 76,
183–191.
4. Md. N. Khan, S. Pal, S. Karamthulla, L. H. Choudhury, RSC Adv., 2014, 4, 3732
 Novel indolizino[8,7-b]indole hybrids as anti-small cell lung cancer
agents: Regioselective modulation of topoisomerase II inhibitory and
DNA crosslinking activities.
1,2
Shahrukhkhan Safi,1,2Wilson Christian, 1,2Dilip Detroja ,1,2Anamik Shah*

1
Department of Chemistry, Saurashtra University, Rajkot-360005, India.
2
Centre of Excellence (CoE), National Facility for Drug Discovery (NFDD) Saurashtra
University, Rajkot-360005, India.
Email:[email protected].

Abstract::A novel series of bis(hydroxymethyl)indolizino[8,7-b]indole hybrids composed of

b-carboline (topoisomerase I/II inhibition) and bis(hydroxymethyl)pyrrole (DNA cross-
linking) are synthesized for antitumor evaluation. Of tumor cell lines tested, small cell lung
cancer (SCLC) cell lines are the most sensitive to the newly synthesized compounds. These
hybrids induce cell cycle arrest at the G2/M phase, trigger tumor cell apoptotic death, and
display diverse mechanisms of action involving topoisomerase II (Topo II) inhibition and
induction of DNA cross-linking. Intriguingly, the substituent at N11 (H or Me) plays a
critical role in modulating Topo II inhibition and DNA cross-linking activities. N11-Me
derivatives predispose to induce DNA crosslinks, whereas N11-H derivatives potently inhibit
Topo II. Computational analysis implicates that N11-Me restrict the torsion angles of the two
adjacent OH on pyrrole resulting in a favorable of DNA cross-linking. Among these hybrids,
compound 17a with N11-H is more effective than cisplatin and etoposide, but as potent as
irinotecan, against the growth of SCLC H526 cells in xenograft model.

Graphical abstract:

Keywords:Anti-SCLC hybrids, b-carboline, bis(hydroxymethyl)pyrrole, indolizino[8,7-

b]indole, DNA cross-linking Topoisomerase inhibition