Compounds > pregna-4-17-diene-3-16-dione--(17z)-isomer

pregna-4-17-diene-3-16-dione--(17z)-isomer and benzamide

pregna-4-17-diene-3-16-dione--(17z)-isomer has been researched along with benzamide* in 1 studies

Other Studies

1 other study(ies) available for pregna-4-17-diene-3-16-dione--(17z)-isomer and benzamide

Article	Year
Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists. Bioorganic & medicinal chemistry, 2015, Oct-01, Volume: 23, Issue:19 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. Topics: Benzamides; Benzoates; Drug Evaluation, Preclinical; Humans; Protein Binding; Receptors, Cytoplasmic and Nuclear; Structure-Activity Relationship	2015

Article

Year

Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists.

Bioorganic & medicinal chemistry, 2015, Oct-01, Volume: 23, Issue:19

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.

Topics: Benzamides; Benzoates; Drug Evaluation, Preclinical; Humans; Protein Binding; Receptors, Cytoplasmic and Nuclear; Structure-Activity Relationship

2015