Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 3, Issue 4, Pages 273-277Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml200256d
Keywords
bile acid; TGR5; avicholic acid; 16-epi-avicholic acid; FXR; structure-activity relationship; CMC
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Funding
- Intercept Pharmaceuticals (New York)
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Grounding on our former 3D QSAR studies, a knowledge-based screen of natural bile acids from diverse animal species has led to the identification of avicholic acid as a selective but weak TGRS agonist. Chemical modifications of this compound resulted in the disclosure of 6 alpha-ethyl-16-epi-avicholic acid that shows enhanced potency at TGRS and FXR receptors. The synthesis, biological appraisals, and structure-activity relationships of this series of compounds are herein described. Moreover, a thorough physicochemical characterization of 6 alpha-ethyl-16-epi-avicholic acid as compared to naturally occurring bile acids is reported and discussed.
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