6α-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity

被引：630

作者：

Pellicciari, R

Fiorucci, S

Camaioni, E

Clerici, C

Costantino, G

Maloney, PR

Morelli, A

Parks, DJ

Willson, TM

机构：

[1] Univ Perugia, Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy

[2] Univ Perugia, Dipartimento Med Clin & Sperimentale, Clin Gastroenterol & Epatol, I-06123 Perugia, Italy

[3] GlaxoSmithKline, Discovery Res, Res Triangle Pk, NC 27709 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 17期

关键词：

D O I：

10.1021/jm025529g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 6alpha-alkyl-substituted analogues of chenodeoxycholic acid (CDCA) were synthesized and evaluated as potential farnesoid X receptor (FXR) ligands. Among them, 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA) was shown to be a very potent and selective FXR agonist (EC50 = 99 nM) and to be endowed with anticholeretic activity in an in vivo rat model of cholestasis.

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页码：3569 / 3572

页数：4

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