In-silico design and synthetic studies of DNA-Gyrase inhibitors: Design, Synthesis and Anti-bacterial activity of 5,7-dihydroxy-4-methylcoumarin derivatives as DNA-gyrase inhibitors

In-silico design and synthetic studies of DNA-Gyrase inhibitors: Design, Synthesis and Anti-bacterial activity of 5,7-dihydroxy-4-methylcoumarin derivatives as DNA-gyrase inhibitors


59,00 €
inkl. MwSt. & Versandkosten (innerhalb Deutschlands)

von Umesh Shiroya, Sanjay Patel, Anand Patel

Beschreibung

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.