1301212-63-4Relevant academic research and scientific papers
STEROID DERIVATIVE FXR AGONIST
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, (2018/12/13)
The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases.
Extending SAR of bile acids as FXR ligands: Discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor- 5β-cholan-23-amine
Gioiello, Antimo,MacChiarulo, Antonio,Carotti, Andrea,Filipponi, Paolo,Costantino, Gabriele,Rizzo, Giovanni,Adorini, Luciano,Pellicciari, Roberto
, p. 2650 - 2658 (2011/06/11)
Within our efforts in the discovery of novel potent and selective ligands for the FXR receptor, 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy- 6α-ethyl-24-nor-5β-cholan-23-amine was synthesized and evaluated for its ability to activate and modulate the biological response of the receptor. Alphascreen and RT-PCR revealed that the 6α-ethyl-24-norcholanyl-23-amine derivate behaves as full FXR agonist endowed with high binding affinity and efficacy, representing a promising lead candidate for further optimization. In addition, docking studies provide new insights into the molecular basis governing the partial and full agonist activity at FXR.
