1,7-Disubstituted oxyindoles are potent and selective EP3 receptor antagonists |
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| Authors: | Nian Zhou 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 |
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| Affiliation: | 1. deCODE Chemistry, 2501 Davey Road, Woodridge, IL 60517, USA;2. deCODE genetics, Inc. Reykjavik, Iceland |
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| Abstract: | A series of novel 1,7-disubstituted oxyindoles were shown to be potent and selective EP3 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, EP1, EP2 and EP4. These agents also featured low CYP inhibition and good activity in the functional rat platelet aggregation assay. |
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