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 MoreWENZHOU M&C FOREIGN TRADE CO.,LTD.
Contact:+86-577-88862917
Address:No.8 Liming West Road,Wenzhou,zhejiang,China
Contact:+86-0311-84455288-844
Address:Mayu Industrial Park, Jinzhou, Hebei, China.
Hangzhou Neway Chemicals Co., Ltd.
Contact:+86-571-85095566
Address:Room 803, Qinglian Bldg, No 139 Qingchun Road, Hangzhou, Zhejiang China
website:http://www.easchem.com
Contact:+86-731-89722861 89722891
Address:2/F-4/Bld Colorful Palace, No.605 Changsha Ave, Yuhua Area Changsha Hunan China.
website:http://www.chinabarton.com
Contact:+86-573-82719618
Address:No. 162 Fumin Road, Honghe Town,
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)