Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.


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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@article{Riendeau2005InhibitorsOT, title={Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.}, author={Denis Riendeau and Ren{\'e}e Aspiotis and Diane Ethier and Yves Gareau and Erich L Grimm and Jocelyne Guay and S{\'e}bastien Guiral and H{\'e}l{\`e}ne J{\^u}teau and Joseph A. Mancini and Nathalie M{\'e}thot and Joel Rubin and Richard W Friesen}, journal={Bioorganic & medicinal chemistry letters}, year={2005}, volume={15 14}, pages={3352-5} }