ResearchBib Share Your Research, Maximize Your Social Impacts
Sign for Notice Everyday Sign up >> Login

DESIGN, SYNTHESIS OF SCHIFF BASE CIPROPFLOXACIN-VANILLIN DERAVATIVES OF POTENT BACTERIAL DNA GYRASE INHIBITOR

Journal: Indian Drugs (Vol.57, No. 03)

Publication Date:

Authors : ; ;

Page : 21-26

Keywords : For Correspondence E-mail: psudhirkumar@soa.ac.in;

Source : Downloadexternal Find it from : Google Scholarexternal

Abstract

A series of Schiff base ciprofloxacin hydrazones with vanillin analogues were designed and validated for druggability properties by advanced computational tools, from which two shortlisted compounds were synthesized and characterized by different spectral studies. These compounds were used against bacterial DNA gyrase; purposedly attempted in molecular docking studies, the compounds 5h and 5i indicated good binding affinity of -8.2 and -8.5 kcal/mol, respectively. Moreover, in vitro antibacterial activities against uropathogenic bacteria, E. coli, was assessed and the compounds 5h, and 5i had significant inhibitory actions. SAR studies revealed that the presence of the quinolone nucleus, azomethine functional group and vanillyl ester might have shown the response of antibacterial inhibition. Thus, vanillyl esters condensed with ciprofloxacin hydrazone through Schiff base, have more antibacterial inhibitory actions. The recorded antibacterial results were corroborated with docking results.

Last modified: 2020-05-15 19:04:29