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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Design, Synthesis and Characterization of N', N'-Diaryl Ureas as p38 Kinase Inhibitors

Author(s): Ravindra G. Kulkarni, Stefan Laufer, Chandrashekhar Mangannavar and Achaiah Garlapati

Volume 9, Issue 2, 2013

Page: [213 - 221] Pages: 9

DOI: 10.2174/1573406411309020006

Price: $65


Kinases have been known as important molecular targets for various diseases and p38 kinase is found to be vital target among all mitogen activated protein kinases for inflammatory diseases. P38 kinase inhibitors bearing urea scaffold have shown potent kinase inhibitory activity and also selectivity over other kinases. We present here the synthesis, p38 kinase inhibitory and anti-inflammatory activities of compounds containing N', N"-diarylurea scaffold. Compound 7f demonstrated IC50 value of 1.09 μM in p38 kinase assay and 79.41% inhibition of rat paw edema at the 2nd hour of carrageenan challenge. The molecular docking studies of synthesized compounds indicated some of the important hydrogen bonding interactions and also revealed the minor change in the binding pose when compared to BIRB796.

Keywords: Ureas/p38 kinase/anti-inflammatory/Docking/BIRB 796

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