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

Autor: McClure KF; Pfizer Global Research and Development, Groton Laboratories, CT 06340, USA. kim.f.mcclure@pfizer.com, Letavic MA, Kalgutkar AS, Gabel CA, Audoly L, Barberia JT, Braganza JF, Carter D, Carty TJ, Cortina SR, Dombroski MA, Donahue KM, Elliott NC, Gibbons CP, Jordan CK, Kuperman AV, Labasi JM, Laliberte RE, McCoy JM, Naiman BM, Nelson KL, Nguyen HT, Peese KM, Sweeney FJ, Taylor TJ, Trebino CE, Abramov YA, Laird ER, Volberg WA, Zhou J, Bach J, Lombardo F
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Aug 15; Vol. 16 (16), pp. 4339-44. Date of Electronic Publication: 2006 Jun 12.
DOI: 10.1016/j.bmcl.2006.05.056
Abstrakt: 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.
Databáze: MEDLINE