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

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.
AuthorsRoberto Pellicciari, Stefano Fiorucci, Emidio Camaioni, Carlo Clerici, Gabriele Costantino, Patrick R Maloney, Antonio Morelli, Derek J Parks, Timothy M Willson
JournalJournal of medicinal chemistry (J Med Chem) Vol. 45 Issue 17 Pg. 3569-72 (Aug 15 2002) ISSN: 0022-2623 [Print] United States
PMID12166927 (Publication Type: Journal Article)
Chemical References
  • Anticholesteremic Agents
  • DNA-Binding Proteins
  • Ligands
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors
  • obeticholic acid
  • farnesoid X-activated receptor
  • Chenodeoxycholic Acid
Topics
  • Animals
  • Anticholesteremic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Line
  • Chenodeoxycholic Acid (analogs & derivatives, chemical synthesis, chemistry, pharmacology)
  • Cholestasis (chemically induced, drug therapy, pathology)
  • DNA-Binding Proteins (agonists)
  • Humans
  • Ligands
  • Liver (drug effects, pathology)
  • Rats
  • Rats, Wistar
  • Receptors, Cytoplasmic and Nuclear
  • Structure-Activity Relationship
  • Transcription Factors (agonists)

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