6α-Ethyl-Chenodeoxycholic Acid (6-ECDCA), a Potent and Selective FXR Agonist Endowed with Anticholestatic Activity

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Authors

Roberto Pellicciari · University of Perugia

Stefano Fiorucci · University of Perugia

Emidio Camaioni · University of Perugia

Carlo Clerici · University of Perugia

Gabriele Costantino · University of Perugia

Patrick Maloney · University of Perugia

Antonio Morelli ·

Abstract

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 (EC(50) = 99 nM) and to be endowed with anticholeretic activity in an in vivo rat model of cholestasis.

Topics & Keywords

Drug Transport and Resistance Mechanisms Cholesterol and Lipid Metabolism Pregnancy and Medication Impact

UN Sustainable Development Goals

Clean water and sanitation

Publication Details

Published in: Journal of Medicinal Chemistry

Volume 45, Issue 17, pp. 3569-3572

DOI: 10.1021/jm025529g

Field-Weighted Citation Impact: 5.41