Bioorganic and Medicinal Chemistry Letters p. 3352 - 3355 (2005)
Update date:2022-08-03
Topics:
Riendeau, Denis
Aspiotis, Renee
Ethier, Diane
Gareau, Yves
Grimm, Erich L.
Guay, Jocelyne
Guiral, Sebastien
Juteau, Helene
Mancini, Joseph A.
Methot, Nathalie
Rubin, Joel
Friesen, Richard W.
A series of potent and selective inhibitors of the inducible microsomal PGE2 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 PGE2 in cell based assays but with a decreased potency and more limited selectivity compared to the enzyme assays.
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