Novel tetrahydrochinoline derived CETP inhibitors.

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

Novel tetrahydrochinoline derived CETP inhibitors.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1740-3. doi: 10.1016/j.bmcl.2010.01.071. Epub 2010 Jan 21.

PubMed ID

20137927 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Torcetrapib	Cholesteryl ester transfer protein	IC 50 (nM)	20	N/A	N/A	Details
Torcetrapib	Cholesteryl ester transfer protein	IC 50 (nM)	18	N/A	N/A	Details
Torcetrapib	Cholesteryl ester transfer protein	IC 50 (nM)	3	N/A	N/A	Details