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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

Bioorg Med Chem Lett · · 4

Schmeck C, Gielen-Haertwig H, Vakalopoulos A, Bischoff H, Li V, Wirtz G, Weber O

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.

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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.