Synthesis, p38 Kinase Inhibitory and Anti-inflammatory Activity of New Substituted Benzimidazole Derivatives

Author(s): Ravindra G. Kulkarnia, Stefan A. Laufer, Chandrashekhar V. M, Achaiah Garlapati

Journal Name: Medicinal Chemistry

Volume 9 , Issue 1 , 2013

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Abstract:

P38 mitogen activated protein kinases have been found to involve in the production and release of unwarranted levels of pro-inflammatory cytokines including TNFα and IL-1β in numerous inflammatory diseases. A new series of molecules, 5-substituted benzoylamino-2-substituted phenylbezimidazoles has been synthesized from 4-nitro-1, 2- diaminobenzene. The synthesized compounds were characterized by FTIR, 1HNMR and Mass. The final compounds were screened for in vitro p38 kinase inhibitory and in vivo anti-inflammatory activity. Three compounds from the series demonstrated nearly 50% inhibition of p38 kinase in the in vitro screening method at 10 M concentration and two molecules exhibited greater than 75% inhibition of paw oedema volume during the first hour. The docking study of synthesized molecule revealed a new binding pose in ATP binding pocket.

Keywords: p38 kinase inhibitors, benzimidazoles, anti-inflammatory activity

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Article Details

VOLUME: 9
ISSUE: 1
Year: 2013
Page: [91 - 99]
Pages: 9
DOI: 10.2174/1573406411309010091

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