Abstract
A series of potent and selective inhibitors of the inducible microsomal PGE 2 synthase (mPGES-1) has been developed based on the indole FLAP inhibitor MK-886. Compounds 23 and 30 inhibit mPGES-1 with potencies in the low nanomolar range and with selectivities of at least 100-fold compared to their inhibition of mPGES-2, thromboxane synthase and binding affinity to FLAP. They also block the production of PGE 2 in cell based assays but with a decreased potency and more limited selectivity compared to the enzyme assays.
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