Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2022 , Vol 26 , Issue 3
Novel pyrazole substituted oxazole derivatives: Design, insilico studies, synthesis & biological activities
1Department of Pharmaceutical Chemistry, Shadan Womens College of Pharmacy, Hyderabad – 500 004, Telangana, India
2Department of Pharmaceutical Chemistry, GITAM Institute of Pharmacy, GITAM (Deemed to be University), Gandhi Nagar, Rushikonda, Visakhapatnam – 530 045, Andhra Pradesh, India
DOI : 10.29228/jrp.160 A potent antibacterial drug was developed by synthesizing a set of new pyrazoles substituted oxazole derivatives using multi-step synthesis. FT-IR, 1H-NMR, Mass spectroscopy, and bases of microanalyses are employed to confirm the structure of compounds. Molinspiration online tool was used to predict the molecular properties and molecular docking was used to predict the antitubercular potency of the target compounds. 10-Fold serial dilution method, agar streak dilution test, and DPPH radical scavenging methods are utilized to evaluate antitubercular, antibacterial, and radical scavenging properties of test compounds and reference drugs, respectively. Varying degree of antitubercular, antibacterial, and radical scavenging activities (mild to good) was displayed by synthesized oxazole compounds. In general, unsubstituted oxazole derivatives exhibited superior antibacterial potency than substituted analogs. In addition, meta-substituted analogs displayed higher activity than the corresponding para-substituted analogs. Among fifteen tested target compounds, the potent compound of this series was found to be 4-(4-(5-phenyl- 4,5-dihydro-1H-pyrazol-3-yl)benzylidene)-2-methyloxazol-5(4H)-one (PBO8). Hence, this analog may be used as a lead molecule to find potent & safer antibacterial agents. Keywords : Oxazole; Pyrazole; Antitubercular activity; Antibacterial activity; Antioxidant activity
Marmara University