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. 2006 Aug 15;16(16):4339-44.
doi: 10.1016/j.bmcl.2006.05.056. Epub 2006 Jun 12.

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

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

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

Kim F McClure et al. Bioorg Med Chem Lett. .

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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