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S-(2-(acylamino)phenyl) 2,2-dimethylpropanethioates as CETP inhibitors
Kimiya Maeda1, Hiroshi Okamoto, Hisashi Shinkai
1Central Pharmaceutical Research Institute, JT Inc., 1-1 Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
Bioorganic & Medicinal Chemistry Letters
|April 28, 2004
Abstract:
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.