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.
View MoreContact:+86-574-87065746
Address:10th Floor, No.787 Baizhang East Road,
Beijing Stable Chemcial Co.ltd
Contact:86-10-63785052
Address:A1301 Technological Edifice. No.4 FuFeng Road,FengTai District, Beijing. China
Contact:+86-025-85553873
Address:Building 27, NO.699-18 XuanWu Avenue, Nanjing, Jiangsu, P.R.China.
Contact:+65 9658 0999
Address:26 Sin Ming Lane, Midview City, #05-118, Singapore 573971
Chengdu Cogon Bio-tech Co., Ltd.
Contact:86-28-85171192
Address:NO.52.YongFeng Rd. Chengdu,610041,P.R.China.
Doi:10.1016/j.tet.2004.04.060
(2004)Doi:10.1016/S0040-4039(01)86315-2
(1979)Doi:10.1039/b613346k
(2007)Doi:10.1002/cber.19791121011
(1979)Doi:10.1016/j.tetlet.2004.04.006
(2004)Doi:10.1021/jo01292a054
(1980)