A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound (12d) has shown an ability to raise HDL significantly in transgenic mouse PD model.
Chromanol derivatives—A novel class of CETP inhibitors
✍ Scribed by Alexandros Vakalopoulos; Carsten Schmeck; Michael Thutewohl; Volkhart Li; Hilmar Bischoff; Klemens Lustig; Olaf Weber; Holger Paulsen; Harry Elias
- Book ID
- 104005060
- Publisher
- Elsevier Science
- Year
- 2011
- Tongue
- English
- Weight
- 305 KB
- Volume
- 21
- Category
- Article
- ISSN
- 0960-894X
No coin nor oath required. For personal study only.
✦ Synopsis
Based on our former development candidate BAY 38-1315, optimization efforts led to the discovery of a novel chemical class of orally active cholesteryl ester transfer protein (CETP) inhibitors. The chromanol derivative 19b is a highly potent CETP inhibitor with favorable pharmacokinetic properties suitable for clinical studies. Chemical process optimization furnished a robust synthesis for a kilogram-scale process.
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