Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.
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Escribano A, Mateo AI, Martin de la Nava EM, Mayhugh DR, Cockerham SL, Beyer TP, Schmidt RJ, Cao G, Zhang Y, Jones TM, Borel AG, Sweetana SA, Cannady EA, Mantlo NB
Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.
Bioorg Med Chem Lett. 2012 Jun 1;22(11):3671-5. doi: 10.1016/j.bmcl.2012.04.042. Epub 2012 Apr 13.
- PubMed ID
- 22543028 [ View in PubMed]
- Abstract
This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and favorable pharmacokinetic properties.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Torcetrapib Cholesteryl ester transfer protein IC 50 (nM) 39 N/A N/A Details