103253-35-6Relevant 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 (2005)
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.
Indole-2-alkanoic acids compositions of and anti allergic use thereof
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, (2008/06/13)
Indole-2-alkanoic acids are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, inflammation, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion and dismenorrhea and as cytoprotective agents.
