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Bioorg Med Chem Lett. 2013 Feb 1;23(3):907-11. doi: 10.1016/j.bmcl.2012.10.040. Epub 2012 Oct 16.

Novel benzoxazole inhibitors of mPGES-1.

Author information

1
Pfizer Research Technology Center, 620 Memorial Dr., Cambridge, MA 02139, USA.

Abstract

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.

PMID:
23266122
DOI:
10.1016/j.bmcl.2012.10.040
[Indexed for MEDLINE]

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