Bioorganic and Medicinal Chemistry p. 6427 - 6436 (2015)
Update date:2022-08-03
Topics:
Song, Kebiao
Xu, Xing
Liu, Peng
Chen, Lili
Shen, Xu
Liu, Junhua
Hu, Lihong
3-(tert-Butyl)-4-hydroxyphenyl 2,4-dichlorobenzoate (1) was discovered in our in-house high throughput screening as a moderate FXR antagonist. To improve the potency and the stability of the hit 1, forty derivatives were synthesized and SAR was systematically explored. The results turn out that replacing the 2,4-dichlorophenyl with 2,6-dichloro-4-amidophenyl shows great improvement in potency, replacing the benzoate with benzamide shows improvement in stability and slight declining of potency and 3-(tert-butyl)-4-hydroxyphenyl unit is essential in obtaining the FXR antagonistic activity.
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