Abstract
Cholesteryl ester transfer protein is a plasma glycoprotein that transfers cholesterol ester between lipoprotein particles. Inhibition of this protein, in vitro and in vivo, produces an increase in plasma high density lipoprotein cholesterol (HDL-C). This communication will describe the SAR and synthesis of a series of substituted tetrahydroquinoxaline CETP inhibitors from early mu lead to advanced enantiomerically pure analogs.
MeSH terms
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Animals
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Chemistry, Pharmaceutical / methods*
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Cholesterol Ester Transfer Proteins / antagonists & inhibitors*
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Cholesterol, HDL / metabolism
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Drug Design
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Esters / chemistry*
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Humans
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Hydrogen-Ion Concentration
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Inhibitory Concentration 50
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Molecular Conformation
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Quinoxalines / chemical synthesis*
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Quinoxalines / pharmacology*
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Rats
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Stereoisomerism
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Structure-Activity Relationship
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Tetrazoles / chemistry*
Substances
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Cholesterol Ester Transfer Proteins
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Cholesterol, HDL
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Esters
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Quinoxalines
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Tetrazoles