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Vol.1/Issue-4/Oct-Dec.2010 International Journal of Pharma and Bio Sciences DESIGN, SYNTHESIS, PHARMACOLOGICAL SCREENING AND MOLECULAR DOCKING OF BIPHENYL ANALOGUES AS ANTIINFLAMMATORY AGENTS

By Shivajirao S. Kadam, Vithal and M. Kulkarni

Abstract

Various direct analogues of flurbriprofen [ 4’-methylbiphenyl-2-(substituted phenyl) carboxamide derivatives] were synthesized and evaluated for anti-inflammatory activity by carrageenan induced rat paw edema model. Compounds 3g, 3h and 3i were found significantly active. Substituents –SO2NH2,-F and-Cl exhibited significant anti-inflammatory activity. Molecular docking was performed using Glide to study the binding mode of these direct analogues of flurbriprofen. The docking analysis of highest active molecule 3g (Glide XP score-8.39) shows significant interaction with active site amino acid residues. Results of this study indicated that these direct analogues of flurbriprofen have affinity towards COX-2 active site which can further be explored as selective COX-2 inhibitors

Topics: Anti-Inflammatory agents, flurbriprofen, Docking
Year: 2011
OAI identifier: oai:CiteSeerX.psu:10.1.1.185.4464
Provided by: CiteSeerX
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