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.
Kablaoui, Natasha,Patel, Snahel,Shao, Jay,Demian, Douglas,Hoffmaster, Keith,Berlioz, Francioise,Vazquez, Michael L.,Moore, William M.,Nugent, Richard A.
p. 907 - 911
(2013/02/25)
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