148693-70-3Relevant academic research and scientific papers
Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886
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.
, p. 3352 - 3355 (2007/10/03)
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.
