| Literature DB >> 15953724 |
Denis Riendeau1, Renee Aspiotis, Diane Ethier, Yves Gareau, Erich L Grimm, Jocelyne Guay, Sébastien Guiral, Hélène Juteau, Joseph A Mancini, Nathalie Méthot, Joel Rubin, Richard W Friesen.
Abstract
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.Entities:
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Year: 2005 PMID： 15953724 DOI： 10.1016/j.bmcl.2005.05.027
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823