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

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  • Engels
  • Paperback
  • 9783848483075
  • 21 april 2012
  • 128 pagina's
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Samenvatting

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.

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Taal
en
Bindwijze
Paperback
Oorspronkelijke releasedatum
21 april 2012
Aantal pagina's
128
Illustraties
Nee

Betrokkenen

Hoofdauteur
Umesh Shiroya
Tweede Auteur
Sanjay Patel
Co Auteur
Patel, Anand

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Extra groot lettertype
Nee
Product breedte
152 mm
Product hoogte
8 mm
Product lengte
229 mm
Studieboek
Ja
Verpakking breedte
152 mm
Verpakking hoogte
8 mm
Verpakking lengte
229 mm
Verpakkingsgewicht
200 g

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EAN
9783848483075

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