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

A series of 6α-alkyl-substituted analogues of chenodeoxycholic acid (CDCA) were synthesized and evaluated as potential farnesoid X receptor (FXR) ligands. Among them, 6α-ethyl-chenodeoxycholic acid (6-ECDCA) was shown to be a very potent and selective FXR agonist (EC50 = 99 nM) and to be endowed wit...

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Veröffentlicht in:Journal of medicinal chemistry 2002-08, Vol.45 (17), p.3569-3572
Hauptverfasser: Pellicciari, Roberto, Fiorucci, Stefano, Camaioni, Emidio, Clerici, Carlo, Costantino, Gabriele, Maloney, Patrick R, Morelli, Antonio, Parks, Derek J, Willson, Timothy M
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Sprache:eng
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Zusammenfassung:A series of 6α-alkyl-substituted analogues of chenodeoxycholic acid (CDCA) were synthesized and evaluated as potential farnesoid X receptor (FXR) ligands. Among them, 6α-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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm025529g