2. Academic Validation
  3. Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors

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

  • Bioorg Med Chem Lett. 2009 May 1;19(9):2386-91. doi: 10.1016/j.bmcl.2009.03.104.
Pier F Cirillo 1,  Eugene R Hickey,  Neil Moss,  Steffen Breitfelder,  Raj Betageri,  Tazmeen Fadra,  Faith Gaenzler,  Thomas Gilmore,  Daniel R Goldberg,  Victor Kamhi,  Thomas Kirrane,  Rachel R Kroe,  Jeffrey Madwed,  Monica Moriak,  Matthew Netherton,  Christopher A Pargellis,  Usha R Patel,  Kevin C Qian,  Rajiv Sharma,  Sanxing Sun,  Alan Swinamer,  Carol Torcellini,  Hidenori Takahashi,  Michele Tsang,  Zhaoming Xiong
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceutical, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA.
PMID: 19356929 DOI: 10.1016/j.bmcl.2009.03.104
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.

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