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New tetrazolyl tetrahydroquinoline CETP inhibitors raise HDL cholesterol in a transgenic mouse model (Bioorg Med Chem Lett 2012)

Original title: Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors

Bioorg Med Chem Lett · · 3

Escribano A, Mateo AI, Martin de la Nava EM, Mayhugh DR, Cockerham SL, Beyer TP, Schmidt RJ, Cao G, Zhang Y, Jones TM, Borel AG, Sweetana SA et al.

This letter describes the discovery and structure-activity relationship optimisation of tetrazolyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m, an exemplar from this series, produced a robust increase in HDL cholesterol in a human CETP and human apolipoprotein A-I double transgenic mouse model, alongside favourable pharmacokinetic properties.

Read the paper (DOI)PubMed

Original abstract

This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and favorable pharmacokinetic properties.

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Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.