1. Academic Validation
  2. Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase

Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2634-8. doi: 10.1016/j.bmcl.2010.02.047.
John K Walker 1 Shaun R Selness Rajesh V Devraj Michael E Hepperle Win Naing Huey Shieh Ravi Kurambail Syaulan Yang Daniel L Flynn Alan G Benson Dean M Messing Tom Dice Tina Kim R J Lindmark Joseph B Monahan Joseph Portanova
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, St. Louis, MO 63017, USA. jkwalker24@sbcglobal.net
Abstract

Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38alpha kinase. Key to this outcome was the switch from a pyridyl to pyrimidine at the C(4)-position leading to analogs that were potent in human whole blood based cell assay as well as in a number of animal efficacy models for rheumatoid arthritis. Ultimately, we identified a clinical candidate from this substrate; SD-0006.

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