Novel tetrahydrochinoline derived CETP inhibitors.
Article Details
- CitationCopy to clipboard
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]
- 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