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Synthesis and biological evaluation of newer analogues of 2,5-disubstituted 1,3,4-oxadiazole containing pyrazole moiety as antimicrobial agents
Institution:1. Medicinal Chemistry Laboratory, Department of Chemistry, National Institute of Technology Karnataka, Surathkal, Mangalore 575025, India;2. Department of Chemistry, KLS Gogte Institute of Technology, Udaymbag, Belgaum 590008, Karnataka, India;3. Department of Bio-Chemistry, Jnanasahyadri, Kuvempu University, Shankaraghatta 577451, Karnataka, India;4. Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia;5. X-ray Crystallography Unit, School of Physics, Universiti Sains Malaysia, Penang 11800, Malaysia
Abstract:A series of 2,5-disubstituted-1,3,4-oxadiazole derivatives bearing pyrazole moiety were synthesized by reacting various substituted pyrazole-4-carboxylic acids with different hydrazides in POCl3. All the synthesized compounds (4a–n) were characterized by IR, NMR, mass spectra and elemental analyses. Synthesized 1,3,4-oxadiazole derivatives were screened for their antibacterial activity against three different strains, namely Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, while antifungal activity was determined against three different strains Aspergillus flavus, Chrysosporium keratinophilum and Candida albicans. The investigation of antimicrobial screening revealed that compounds 4i and 4j exhibited excellent activity when compared with the standard drugs.
Keywords:Antimicrobial activity  1  3  4-Oxadiazoles  Pyrazoles
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