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.
Tags: Medizin, Pharmazie
Taschenbuch - 9783848483075 Verlag: LAP Lambert Academic Publishing Ersterscheinung: April 2012 ISBN-13: 9783848483075 Größe: 220 mm x 150 mm x 8 mm Gewicht: 207 Gramm 128 Seiten Versandfertig in 3-5 Tagen.