In-silico design and synthetic studies of DNA-Gyrase inhibitors

In-silico design and synthetic studies of DNA-Gyrase inhibitors

EnglishPaperback / softbackPrint on demand
Shiroya, Umesh
LAP Lambert Academic Publishing
EAN: 9783848483075
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Detailed information

Coumarins are important class of compounds, isomeric to quinolones. They may become promising candidates for exploiting more useful therapeutically active molecules. DNA-gyrase has drawn much attention as selected target for finding potent anti-bacterial agents against multi-drug resistant strains such as methicillin-resistant Staphyloccus aureus (MRSA), vancomycin-resistant enterococci (VRE), penicillin-resistant Streptococci pneumonia (PRSP). The objective of the present study was, to study the molecular docking simulations on 5,7-dihydroxy-4-methyl coumarin analogues as probable candidates for inhibiting DNA gyrase subunit-B of S.aureus. In the present study, Docking simulations were carried out on the reported inhibitors of DNA-gyrase subunit A and B using docking software. Based on it, Series of 5,7-dihydroxy-4-methylcoumarin analogues (PH-1 to PH-9) were designed, synthesized, characterized and evaluated for its anti-bacterial activity against S.aureus and E.coli. Out of the nine test compounds, compound PH-4 showed good anti-bacterial activity against S.aureus and E.coli than rest of other compounds.
EAN 9783848483075
ISBN 3848483076
Binding Paperback / softback
Publisher LAP Lambert Academic Publishing
Publication date April 21, 2012
Pages 128
Language English
Dimensions 229 x 152 x 8
Country Germany
Readership General
Authors Patel, Anand; Patel, Sanjay; Shiroya, Umesh
Edition Aufl.