1. Academic Validation
  2. New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site

New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site

  • Bioorg Med Chem Lett. 2007 Aug 1;17(15):4242-7. doi: 10.1016/j.bmcl.2007.05.042.
Neil Moss 1 Steffen Breitfelder Raj Betageri Pier F Cirillo Tazmeen Fadra Eugene R Hickey Thomas Kirrane Rachel R Kroe Jeffrey Madwed Richard M Nelson Christopher A Pargellis Kevin C Qian John Regan Alan Swinamer Carol Torcellini
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceutical, Inc., 900 Ridgebury Road, Ridgefield, CT 0687, USA. nmoss@rdg.boehringeringleheim.com
Abstract

Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of this particular scaffold. Modification to the part of the inhibitor that occupies the adenine/ATP binding site has resulted in a new way to obtain potent inhibitors that possess favorable in vitro and in vivo properties.

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