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In-silico design and synthetic studies of DNA-Gyrase inhibitors

Autor Umesh Shiroya, Sanjay Patel, Anand Patel
en Limba Engleză Paperback – 20 apr 2012
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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Specificații

ISBN-13: 9783848483075
ISBN-10: 3848483076
Pagini: 128
Dimensiuni: 152 x 229 x 8 mm
Greutate: 0.2 kg
Editura: LAP LAMBERT ACADEMIC PUBLISHING AG & CO KG
Colecția LAP Lambert Academic Publishing

Notă biografică

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.