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Jagani C.L.,Sardar Patel University | Vanparia S.F.,Sardar Patel University | Patel T.S.,Sardar Patel University | Dixit R.B.,Ashok and Rita Patel Institute of Integrated Studies and Research in Biotechnology and Allied science | Dixit B.C.,Sardar Patel University
Arkivoc | Year: 2012

An optimization of the reaction conditions in solvent free and solution phase microwave assisted synthesis of 2-styryl-4(3H)-quinazolinone derivatives having substituted benzothiazole/5-tert-butylisoxazole at the 3rd position is discussed. In solvent free reactions acidic alumina was used as a solid support, while a mixture of DMF and pyridine was used in solution phase synthesis. A comparative study of yield and reaction time for both the optimized method revealed that the solution phase microwave irradiation gave better results than solvent free method. © ARKAT-USA, Inc.

Patel T.S.,Sardar Patel University | Vanparia S.F.,Sardar Patel University | Gandhi S.A.,Sardar Patel University | Patel U.H.,Sardar Patel University | And 3 more authors.
New Journal of Chemistry | Year: 2015

An optimization and modification of Grimmel's method leading to cyclization and incorporation of glycine linked sulphonamide at position-2 in 4-quinazolin-(3H)-ones was accomplished. Generation of a lipophilic site at position-3 of 4-quinazolinones was explored by synthesis of imines, unfortunately leading to an isomeric mixture of stereoisomers. These stereoisomeric mixtures were further converted to a single isomer utilizing the novel methodology developed by the use of an aprotic solvent system. Moreover, a mixture of (Z)/(E)-isomers and single configuration was identified and ascertained using NMR, HMQC, HMBC and NOESY spectroscopic techniques. The synthesized entities were further screened for their antimalarial efficacy pertaining two active scaffolds 8m and 8s. The active molecules were sent forth for enzyme inhibitory study against presumed receptors h-DHFR and Pf-DHFR computationally as well as in vitro, proving their potency as dihydrofolate reductase inhibitors. The oral bioavailability of these active molecules was also predicted by the study of ADME properties, indicating good bioavailability of the active entities. © The Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2015.

Pagedar A.,National Dairy Research Institute | Pagedar A.,Ashok and Rita Patel Institute of Integrated Studies and Research in Biotechnology and Allied science | Singh J.,National Dairy Research Institute | Singh J.,Product and Process Development Group | Batish V.K.,National Dairy Research Institute
Journal of Dairy Research | Year: 2012

The present study investigates the effect of adaptive resistance to ciprofloxacin (Cip) and benzalkonium chloride (BC) on biofilm formation potential (BFP), efflux pump activity (EPA) and haemolysin activity of Escherichia coli isolates of dairy origin. All the isolates, irrespective of antimicrobial susceptibility, developed significant adaptive resistance (P < 0•05). All the resistant phenotypes (antibiotic resistant: AR; & biocide resistant: BR) were stronger biofilm former and post-adaptation, an insignificant change was observed in their BFP. Whereas, post-adaptation, non-resistant isolates (antibiotic non-resistant: ANR; biocide non-resistant: BNR) transformed from poor or moderate to strong biofilm formers. Post-adaptive percentage increase in EPA was highly significant in non-resistant categories (P < 0•01) and significant at P < 0•05 in BR category. Interestingly, post-adaptive increase in EPA in BR isolates was more than that in AR yet, the latter exhibited greater adaptive resistance than the former. These findings indicated prevalence of some other specific resistance mechanism/s responsible for adaptive resistance against Cip. Strain specific variations were observed for stability of adaptive resistance and haemolysin activity for all the categories. Our findings especially in reference to post-adaptation upgradation of BFP status of non-resistant isolates seems to be providing an insight into the process of conversion of non-resistant isolate into resistant ones with enhanced BFP. These observations emphasize the serious implications of sub-lethal residual levels of antimicrobials in food environments and suggest a role of food chain in emergence of antimicrobial resistances. © 2012 Proprietors of Journal of Dairy Research.

Ishnava K.B.,Ashok and Rita Patel Institute of Integrated Studies and Research in Biotechnology and Allied science | Chauhan K.H.,Ashok and Rita Patel Institute of Integrated Studies and Research in Biotechnology and Allied science | Bhatt C.A.,Ashok and Rita Patel Institute of Integrated Studies and Research in Biotechnology and Allied science
Archives of Phytopathology and Plant Protection | Year: 2012

The present study was designated to evaluate the antifungal activity and to root out the antifungal plant leaf extracts from this Indian folk-flore. The in vitro antifungal assay was performed by agar diffusion test and minimum inhibitory concentration (MIC) for hexane, ethyl acetate, methanol and distilled water plant leaf extracts. Extraction of 17 different plant leaves was carried out in different solvents such as hexane, ethyl acetate, methanol and distilled water. Among them extractive yield of methanol was maximum than the rest of the three solvents. These extracts were screened for their antifungal activity against nine different fungi. Among these ethyl acetate extracts of Adhatoda vasica, Ocimum sanctum and Holoptelea integrifolia exhibited maximum antifungal activity against Alternaria sp., Aspergillus parasi, Aspergillus nidulans, Trichoderma harzianum and Aspergillus flavus with MIC of 80, 40 and 20 ppm against Aspergillus nidulans and Alternaria sp. Ethyl acetate extracts showed promising antifungal activity against Adhatoda vasica, Ocimum sanctum and Holoptelea integrifolia against Aspergillus nidulans, and Alternaria sp. might be applicable as fungicide against fungal plants disease. © 2012 Copyright Taylor and Francis Group, LLC.

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