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. 2010 Apr 15;20(8):2658-64.
doi: 10.1016/j.bmcl.2010.02.028. Epub 2010 Feb 25.

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

Nian Zhou  1 , Alexandre M Polozov, Matthew O'Connell, James Burgeson, Peng Yu, Wayne Zeller, Jun Zhang, Emmanuel Onua, Jose Ramirez, Gudrun A Palsdottir, Gudrun V Halldorsdottir, Thorkell Andresson, Alex S Kiselyov, Mark Gurney, Jasbir Singh
Affiliations

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

Nian Zhou et al. Bioorg Med Chem Lett. .

Abstract

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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