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In-silico design and synthetic studies of DNA-Gyrase inhibitors
Umesh Shiroya • Sanjay Patel • Anand Patel
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Uppskattad leveranstid 7-11 arbetsdagar
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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.
- Format: Pocket/Paperback
- ISBN: 9783848483075
- Språk: Engelska
- Antal sidor: 128
- Utgivningsdatum: 2012-04-21
- Förlag: LAP Lambert Academic Publishing