In-Silico Design and Synthetic Studies of DNA-Gyrase Inhibitors

In-Silico Design and Synthetic Studies of DNA-Gyrase Inhibitors

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By (author) Umesh Shiroya, By (author) Sanjay Patel, By (author) Anand Patel

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  • Publisher: LAP Lambert Academic Publishing
  • Format: Paperback | 128 pages
  • Dimensions: 152mm x 229mm x 8mm | 200g
  • Publication date: 21 April 2012
  • ISBN 10: 3848483076
  • ISBN 13: 9783848483075
  • Illustrations note: black & white illustrations

Product description

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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I have got M.pharma (Pharmaceutical chemistry) degree from Gujarat Technological University in 2011.I have worked in different areas of Pharmaceutical field. I have published many research and review articles in reputed journals of chemistry.I have depth knowledge of computational, medicinal and organic chemistry.