1440142-00-6Relevant articles and documents
Synthesis, p38 kinase inhibitory and anti-inflammatory activity of new substituted benzimidazole derivatives
Kulkarni, Ravindra G.,Laufer, Stefan A.,Chandrashekhar,Garlapati, Achaiah
, p. 91 - 99 (2013/04/23)
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 50percent inhibition of p38 kinase in the in vitro screening method at 10 μM concentration and two molecules exhibited greater than 75percent inhibition of paw oedema volume during the first hour. The docking study of synthesized molecule revealed a new binding pose in ATP binding pocket.
