The class
Tetrazole and ester substituted tetrahydroquinoxalines emerge as a potent new class of CETP inhibitors (Bioorg Med Chem Lett 2007)
Original title: Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors
Medicinal chemists describe the structure-activity relationships and synthesis of a series of substituted tetrahydroquinoxaline CETP inhibitors, tracing the chemotype's evolution from an early micromolar lead to advanced enantiomerically pure analogs. Since inhibiting CETP, the plasma glycoprotein that transfers cholesteryl ester between lipoprotein particles, raises plasma HDL cholesterol both in vitro and in vivo, this new tetrazole and ester substituted tetrahydroquinoxaline scaffold adds a structurally distinct chemotype to the CETP inhibitor development pipeline of the mid-2000s.
Original 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.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.