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Current Enzyme Inhibition

Editor-in-Chief

ISSN (Print): 1573-4080
ISSN (Online): 1875-6662

Anti-inflammatory Activities of Phenoxyphenyl Ureas Mediated by Inhibition of p38 Kinase

Author(s): Ravindra Kulkarni, Swapna Diwyani, Stefan Laufer, Chandrshekar V. M., Achaiah G., Prashant Gurav and Prasanna Habbu

Volume 11 , Issue 2 , 2015

Page: [116 - 123] Pages: 8

DOI: 10.2174/1573408011666150729221843

Price: $65

Sekisui-XenoTech-CEI
Abstract

P38 kinase has been known to be one of the important and validated targets for inflammatory diseases including rheumatoid arthritis for its vital role in production and release of proinflammatory cytokines including tumor necrosis factor alpha (TNF-α) and interleukin-beta (IL-1β). Pyridinyl group of our reported compounds was replaced by simple phenyl groups and compounds were synthesized and characterized. A dose of 50 mg/Kg has been administered and observed antiinflammatory activity in rats. Compounds 6h, 6i, 6j and 6o exhibited significant antiinflammatory activity at 3rd hour of carrageenan administration. Compounds 6c, 6j, 6k and others demonstrated greater than 50% p38 kinase inhibitory activity at 10 μM.

Keywords: Anti-inflammatory, diphenyl urea, p38 kinase, synthesis/in vitro/in vivo.

Graphical Abstract

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