RGD Reference Report - 1,7-Disubstituted oxyindoles are potent and selective EP(3) receptor antagonists. - Rat Genome Database

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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.
RGD ID: 10043327
Pubmed: PMID:20303752   (View Abstract at PubMed)
DOI: DOI:10.1016/j.bmcl.2010.02.028   (Journal Full-text)

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.

Objects referenced in this article
Gene Ptger3 prostaglandin E receptor 3 Rattus norvegicus

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