Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 15, Issue 14, Pages 3352-3355Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.05.027
Keywords
prostaglandin synthase; FLAP inhibitors; MK-886; prostaglandin E2; inflammation
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A series of potent and selective inhibitors of the inducible microsomal PGE(2) 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 PGE(2) in cell based assays but with a decreased potency and more limited selectivity compared to the enzyme assays. (c) 2005 Elsevier Ltd. All rights reserved.
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