Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template

Jane Wang, David Limburg, Jeff Carter, Gabriel Mbalaviele, James Gierse, Michael Vazquez

Research output: Contribution to journalArticlepeer-review

58 Scopus citations

Abstract

Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE2 inhibition in a cell-based assay (0.42 μM) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF.

Original languageEnglish
Pages (from-to)1604-1609
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number5
DOIs
StatePublished - Mar 1 2010

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