Abstract Based on structure-based drug design strategy, the optimal compound 2 (EC50=2.43 μM) has been designed and identified. Compound 2 revealed considerable activity on FXR, and exerts best therapeutic effects on alleviating acetaminophen-induced liver damages in this series by up-regulation of FXR-related gene expression in vivo. These results suggest that compound 2 is a promising FXR agonist suitable for further evaluation. Abstract Farnesoid X receptor (FXR) plays an important role in regulating glucolipid metabolism, detoxification,...
