Synthesis and Characterization of Chlorophenylthiazolocoumarinyl Hydrazides as Promising Antimicrobial and Anti-Inflammatory Agents
Journal Title: IOSR Journal of Applied Chemistry (IOSR-JAC) - Year 2018, Vol 11, Issue 7
Abstract
Recently the reports of resistance to antibacterial drugs have drastically increased. In the search of novel antimicrobial agents, green facile synthesis of substituted phenyl-thiazolocoumarinyl hydrazides was designed and achieved by one-pot reaction of substituted 4-formylcoumarin, thiosemicarbazide, and various phenacyl bromides. The substituted phenyl-thiazolocoumarinyl hydrazides were evaluated preliminarily for their antimicrobial and anti-inflammatory activities. The title compounds have shown excellent in vitro antibacterial activity against the S. aureus and E. coli bacterial strains with the value of low MIC ranges from 0.4 to 6.25µg/mL. In vitro antifungal activity of compounds against fungal strains A. niger and A. flavus was found to be excellent as compared with the standard fluconazole with the MIC in the range of 0.4 to 3.12 µg/mL. Substituted phenyl-thiazolocoumarinyl hydrazides have shown potent anti-inflammatory activity against both MMP-2 and MMP-9 by gelatinase zymography compared with the standard drug as tetracycline. Docking study was performed for compounds with S. aureus DNA gyrase.
Authors and Affiliations
Farzanabi Shaikh, Samundeeswari S, Rashmi Kulkarni, Nirmala S. Naik, Jyoti M. Madar, Shrinivas D. Joshi, Vinay Sunagar, Lokesh Shastri
Keywords
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- EP ID EP414335
- DOI 10.9790/5736-1107020939.
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