Research Article | Volume: 7, Issue: 10, October, 2017

Synthesis, Pharmacological Evaluation, Molecular Docking and in silico ADMET Prediction of Nitric Oxide Releasing Biphenyls as Anti-Inflammatory Agents

Monika G. Shinde Siddharth J. Modi Vithal M. Kulkarni   

Open Access   

Published:  Oct 30, 2017

DOI: 10.7324/JAPS.2017.71006
Abstract

Various 2-(4'-methyl-N-phenyl substituted)-1,1'-biphenyl-2-ylcarboxamido-2-oxoethyl nitrate analogues were synthesized and evaluated for analgesic, anti-inflammatory, ulcerogenic activity and nitric oxide release study. Compounds VM-4, VM-6, VM-9, VM-10, VM-11 and VM-12 exhibited good analgesic and anti-inflammatory activity compared to standard drug diclofenac. The compounds also showed decreased gastro-intestinal ulcerogenicity and gastro-protective activity in histopathological studies resulting in absence of mucosal injury. All the synthesized compounds were found to have significant in vivo nitric oxide releasing activity. The molecular docking was performed to understand the binding mode of these compounds. Results of this study indicated that these NO-NSAIDs may have affinity towards COX-2 active site which can further be explored for selective or non-selective inhibitors.


Keyword:     Biphenyl derivatives Docking ADMET Anti-inflammatory activity.


Citation:

Shinde MG, Modi SJ, Kulkarni VM. Synthesis, Pharmacological Evaluation, Molecular Docking and in silico ADMET Prediction of Nitric Oxide Releasing Biphenyls as Anti-Inflammatory Agents. J App Pharm Sci, 2017; 7 (10): 037-047.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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