2. Academic Validation
  3. Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development

Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development

  • Bioorg Med Chem Lett. 2006 Aug 15;16(16):4339-44. doi: 10.1016/j.bmcl.2006.05.056.
Kim F McClure 1,  Michael A Letavic,  Amit S Kalgutkar,  Christopher A Gabel,  Laurent Audoly,  John T Barberia,  John F Braganza,  Demetrius Carter,  Thomas J Carty,  Santo R Cortina,  Mark A Dombroski,  Kathleen M Donahue,  Nancy C Elliott,  Colleen P Gibbons,  Crystal K Jordan,  Alexander V Kuperman,  Jeff M Labasi,  Ronald E Laliberte,  Jennifer M McCoy,  Brian M Naiman,  Kendra L Nelson,  Hang T Nguyen,  Kevin M Peese,  Francis J Sweeney,  Timothy J Taylor,  Catherine E Trebino,  Yuriy A Abramov,  Ellen R Laird,  Walter A Volberg,  Jun Zhou,  Justin Bach,  Franco Lombardo
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Groton Laboratories, CT 06340, USA. kim.f.mcclure@pfizer.com
PMID: 16759861 DOI: 10.1016/j.bmcl.2006.05.056
Abstract

The synthesis, structure-activity relationship, in vivo activity, and metabolic profile for a series of triazolopyridine-oxazole based p38 inhibitors are described. The deficiencies of the lead structure in the series, CP-808844, were overcome by changes to the C4 aryl group and the triazole side-chain culminating in the identification of several potential clinical candidates.

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