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Bioorg Med Chem Lett. 2009 May 1;19(9):2386-91. doi: 10.1016/j.bmcl.2009.03.104. Epub 2009 Mar 26.

Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.

Author information

1
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceutical, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA.

Abstract

An effort aimed at exploring structural diversity in the N-pyrazole-N'-naphthylurea class of p38 kinase inhibitors led to the synthesis and characterization of N-phenyl-N'-naphthylureas. Examples of these compounds displayed excellent inhibition of TNF-alpha production in vitro, as well as efficacy in a mouse model of lipopolysaccharide induced endotoxemia. In addition, perspective is provided on the role of a sulfonamide functionality in defining inhibitor potency.

PMID:
19356929
DOI:
10.1016/j.bmcl.2009.03.104
[Indexed for MEDLINE]

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