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

Roberto Pellicciari; Stefano Fiorucci; Emidio Camaioni; Carlo Clerici; Gabriele Costantino; Patrick Maloney; Antonio Morelli; Derek J. Parks; Timothy M. Willson

doi:10.1021/jm025529g

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

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(University of Perugia), Derek J. Parks(University of Perugia), Timothy M. Willson(University of Perugia)

Journal of Medicinal Chemistry

July 20, 2002

10.1021/jm025529g

Cited by 730Open Access

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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.

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