S-(2-(acylamino)phenyl) 2,2-dimethylpropanethioates as CETP inhibitors.
Studies on the relationship between the structure of the benzene moiety of S-(2-(acylamino)phenyl) 2,2-dimethylpropanethioates and CETP inhibitory activity were performed. Substituents on the benzene moiety influenced CETP inhibitory activity in a type and position dependent manner, and electron-withdrawing groups at the 4- or 5-position increased the activity. The most potent compound showed 50% inhibition of CETP activity in human plasma at a concentration of 2 microM.
Maeda
Kimiya
K
Central Pharmaceutical Research Institute, JT Inc., 1-1 Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Okamoto
Hiroshi
H
Shinkai
Hisashi
H
D000577:Amides; D001161:Arteriosclerosis / Q000517:prevention & control; D002352:Carrier Proteins / Q000037:antagonists & inhibitors* / Q000097:blood; D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL / Q000819:agonists; D004952:Esters; D006023:Glycoproteins / Q000037:antagonists & inhibitors* / Q000097:blood; D006801:Humans; D020128:Inhibitory Concentration 50; D020011:Protective Agents / Q000138:chemical synthesis / Q000494:pharmacology; D011804:Quinolines; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis / Q000494:pharmacology*
D000577:Amides; C506642:CETP protein, human; D002352:Carrier Proteins; D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL; D004952:Esters; D006023:Glycoproteins; D020011:Protective Agents; D011804:Quinolines; D013438:Sulfhydryl Compounds; C411602:dalcetrapib; C483909:torcetrapib