37405-22-4Relevant academic research and scientific papers
A kind of the second aryl amine derivative and its preparation method, pharmaceutical composition and use thereof
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Paragraph 0164; 0166; 0167, (2017/08/30)
The invention provides diarylamide type derivatives having a structure shown as a formula (I) as follows, or pharmaceutically acceptable salts thereof, a preparing method of the derivatives, compositions containing the derivatives and the pharmaceutically acceptable salts, and medicine uses of the derivatives and the pharmaceutically acceptable salts. The diarylamide type derivatives having the structure shown as the formula (I) or the pharmaceutically acceptable salts thereof have antagonistic effects on FXR. Integral animal experiments show that the compounds have effects of decreasing blood sugar and reducing blood fat. The compounds can be used for treating hyperlipidemia and type 2 diabetes mellitus.
Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists
Song, Kebiao,Xu, Xing,Liu, Peng,Chen, Lili,Shen, Xu,Liu, Junhua,Hu, Lihong
, p. 6427 - 6436 (2015/10/05)
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.
