| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1363383 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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.
Graphical abstractVariations in the 4-position of 4 led to novel CETP inhibitors. The cyclohexyl group was found to be a suitable replacement for the pF-phenyl substituent. Compound 11b was identified as a potent CETP inhibitor with an excellent in vitro and PK-profile.Figure optionsDownload full-size imageDownload as PowerPoint slide
