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.
MeSH terms
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Amides
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Arteriosclerosis / prevention & control
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Carrier Proteins / antagonists & inhibitors*
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Carrier Proteins / blood
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Cholesterol Ester Transfer Proteins
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Cholesterol, HDL / agonists
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Esters
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Glycoproteins / antagonists & inhibitors*
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Glycoproteins / blood
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Humans
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Inhibitory Concentration 50
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Protective Agents / chemical synthesis
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Protective Agents / pharmacology
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Quinolines
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Structure-Activity Relationship
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Sulfhydryl Compounds / chemical synthesis
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Sulfhydryl Compounds / pharmacology*
Substances
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Amides
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CETP protein, human
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Carrier Proteins
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Cholesterol Ester Transfer Proteins
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Cholesterol, HDL
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Esters
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Glycoproteins
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Protective Agents
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Quinolines
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Sulfhydryl Compounds
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dalcetrapib
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torcetrapib