1,7-二取代氧化吲哚是强效且选择性的EP(3)受体拮抗剂。
1,7-Disubstituted oxyindoles are potent and selective EP(3) receptor antagonists.
作者信息
Zhou Nian, Polozov Alexandre M, O'Connell Matthew, Burgeson James, Yu Peng, Zeller Wayne, Zhang Jun, Onua Emmanuel, Ramirez Jose, Palsdottir Gudrun A, Halldorsdottir Gudrun V, Andresson Thorkell, Kiselyov Alex S, Gurney Mark, Singh Jasbir
机构信息
deCODE Chemistry, Woodridge, IL 60517, USA.
出版信息
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2658-64. doi: 10.1016/j.bmcl.2010.02.028. Epub 2010 Feb 25.
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.
一系列新型的1,7-二取代氧化吲哚被证明是强效且选择性的EP(3)受体拮抗剂。吲哚C-3位取代模式的变化增强了所得衍生物的体外代谢稳定性。系列27a - c对包括IP、FP、EP(1)、EP(2)和EP(4)在内的一组前列腺素受体表现出超过1000倍的选择性。这些药物在功能性大鼠血小板聚集试验中还具有低CYP抑制作用和良好活性。
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