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Bioorg Med Chem Lett
; 23(3): 907-11, 2013 Feb 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-23266122
RESUMEN
A novel series of potent benzoxazole mPGES-1 inhibitors has been derived from a hit from a high throughput screen. Compound 37 displays mPGES-1 inhibition in an enzyme assay (0.018 µM) and PGE-2 inhibition in a cell-based assay (0.034 µM). It demonstrates 500- and 2500-fold selectivity for mPGES-1 over COX-2 and 6-keto PGF-1α, respectively. In vivo PK studies in dogs demonstrate 55% oral bioavailability and an 7 h half-life.