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Novel tetrahydrochinoline derivatives yield a potent CETP inhibitor with favourable pharmacokinetics for clinical development (Bioorg Med Chem Lett 2010)
Original title: Novel tetrahydrochinoline derived CETP inhibitors
Continuing efforts to identify orally active CETP inhibitors, researchers explored tetrahydrochinoline derivatives based on structural modifications of BAY 19-4789, leading to the discovery of novel cycloalkyl-substituted compounds. Example compound 11b emerged as a highly potent CETP inhibitor both in vitro and in vivo in transgenic mice, with pharmacokinetic properties favourable for further clinical development.
Original abstract
In the course of our efforts to identify orally active cholesteryl ester transfer protein (CETP) inhibitors, we have continued to explore tetrahydrochinoline derivatives. Based on BAY 19-4789 structural modifications led to the discovery of novel cycloalkyl substituted compounds. Thus, example 11b is a highly potent CETP inhibitor both in vitro and in vivo in transgenic mice with favourable pharmacokinetic properties for clinical development.
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Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.