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.
Current Enzyme Inhibition
Title:Anti-inflammatory Activities of Phenoxyphenyl Ureas Mediated by Inhibition of p38 Kinase
Volume: 11 Issue: 2
Author(s): Ravindra Kulkarni, Swapna Diwyani, Stefan Laufer, Chandrshekar V. M., Achaiah G., Prashant Gurav and Prasanna Habbu
Affiliation:
Keywords: Anti-inflammatory, diphenyl urea, p38 kinase, synthesis/in vitro/in vivo.
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.
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Kulkarni Ravindra, Diwyani Swapna, Laufer Stefan, V. M. Chandrshekar, G. Achaiah, Gurav Prashant and Habbu Prasanna, Anti-inflammatory Activities of Phenoxyphenyl Ureas Mediated by Inhibition of p38 Kinase, Current Enzyme Inhibition 2015; 11 (2) . https://dx.doi.org/10.2174/1573408011666150729221843
DOI https://dx.doi.org/10.2174/1573408011666150729221843 |
Print ISSN 1573-4080 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6662 |
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