2444-27-1Relevant articles and documents
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.
Oxidation of Alkoxyphenols. Part 28. On the Configuration of 2,2'-Diphenoquinones
Hewgill, Frank R.,Greca, Bart La,Legge, Frank,Roga, Peter E.
, p. 131 - 134 (2007/10/02)
The n.m.r. spectra of a number of 2,2'-diphenoquinones imply that they have the trans-configuration.The importance of charge-separated structures in unsymmetrical quinones is discussed in relation to the formation of oxepinobenzofurans.
