1,7-Disubstituted oxyindoles are potent and selective EP(3) receptor antagonists.

Authors: Zhou, N  Polozov, AM  O'Connell, M  Burgeson, J  Yu, P  Zeller, W  Zhang, J  Onua, E  Ramirez, J  Palsdottir, GA  Halldorsdottir, GV  Andresson, T  Kiselyov, AS  Gurney, M  Singh, J 
Citation: Zhou N, etal., Bioorg Med Chem Lett. 2010 Apr 15;20(8):2658-64. doi: 10.1016/j.bmcl.2010.02.028. Epub 2010 Feb 25.
Pubmed: (View Article at PubMed) PMID:20303752
DOI: Full-text: DOI:10.1016/j.bmcl.2010.02.028

A series of novel 1,7-disubstituted oxyindoles were shown to be potent and selective EP(3) receptor antagonists. Variation of substitution pattern at the C-3 position of indole enhanced in vitro metabolic stability of the resulting derivatives. Series 27a-c showed >1000-fold selectivity over a panel of prostanoid receptors including IP, FP, EP(1), EP(2) and EP(4). These agents also featured low CYP inhibition and good activity in the functional rat platelet aggregation assay.

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CRRD ID: 10043327
Created: 2015-05-21
Species: All species
Last Modified: 2015-05-21
Status: ACTIVE



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RGD is funded by grant HL64541 from the National Heart, Lung, and Blood Institute on behalf of the NIH.