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

Journal of Medicinal Chemistry · 2002 · Vol. 45(17) · pp. 3569–3572

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)

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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.

Drug Transport and Resistance Mechanisms Cholesterol and Lipid Metabolism Pregnancy and Medication ImpactChenodeoxycholic acidFarnesoid X receptorChemistryAgonistBile acidIn vivoCholestasisReceptorInternal medicinePharmacology

MeSH terms

Receptor, Farnesoid X-ActivatedAnimalsAnticholesteremic AgentsCell LineChenodeoxycholic AcidCholestasisDNA-Binding ProteinsHumansLigandsLiverStructure-Activity RelationshipTranscription FactorsRats, WistarReceptors, Cytoplasmic and NuclearRats

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725

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5.39

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96%

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Bile Acids: Chemistry, Pathochemistry, Biology, Pathobiology, and Therapeutics