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.
  • Views 138
  • Downloads 0

How To Cite

Farzanabi Shaikh, Samundeeswari S, Rashmi Kulkarni, Nirmala S. Naik, Jyoti M. Madar, Shrinivas D. Joshi, Vinay Sunagar, Lokesh Shastri (2018). Synthesis and Characterization of Chlorophenylthiazolocoumarinyl Hydrazides as Promising Antimicrobial and Anti-Inflammatory Agents. IOSR Journal of Applied Chemistry (IOSR-JAC), 11(7), 9-39. https://europub.co.uk/articles/-A-414335