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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Authors | Roberto Pellicciari, Stefano Fiorucci, Emidio Camaioni, Carlo Clerici, Gabriele Costantino, Patrick R Maloney, Antonio Morelli, Derek J Parks, Timothy M Willson |
Journal | Journal of medicinal chemistry
(J Med Chem)
Vol. 45
Issue 17
Pg. 3569-72
(Aug 15 2002)
ISSN: 0022-2623 [Print] United States |
PMID | 12166927
(Publication Type: Journal Article)
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Chemical References |
- Anticholesteremic Agents
- DNA-Binding Proteins
- Ligands
- Receptors, Cytoplasmic and Nuclear
- Transcription Factors
- obeticholic acid
- farnesoid X-activated receptor
- Chenodeoxycholic Acid
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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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