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Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development |
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| Authors: | McClure Kim F Letavic Michael A Kalgutkar Amit S Gabel Christopher A Audoly Laurent Barberia John T Braganza John F Carter Demetrius Carty Thomas J Cortina Santo R Dombroski Mark A Donahue Kathleen M Elliott Nancy C Gibbons Colleen P Jordan Crystal K Kuperman Alexander V Labasi Jeff M Laliberte Ronald E McCoy Jennifer M Naiman Brian M Nelson Kendra L Nguyen Hang T Peese Kevin M Sweeney Francis J Taylor Timothy J Trebino Catherine E Abramov Yuriy A Laird Ellen R Volberg Walter A Zhou Jun Bach Justin Lombardo Franco |
| Affiliation: | Pfizer Global Research and Development, Groton Laboratories, CT 06340, USA. kim.f.mcclure@pfizer.com |
| 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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