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Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase |
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| Authors: | John K Walker 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 RJ Lindmark Joseph B Monahan Joseph Portanova |
| Institution: | Pfizer Global Research and Development, Chesterfield Parkway West, St. Louis, MO 63017, USA |
| Abstract: | Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38α 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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