1 research outputs found
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators
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 TGR5
agonist. Chemical modifications of this compound resulted in the disclosure
of 6α-ethyl-16-<i>epi</i>-avicholic acid that shows
enhanced potency at TGR5 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 6α-ethyl-16-<i>epi</i>-avicholic
acid as compared to naturally occurring bile acids is reported and
discussed