Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.

Article Details

Citation

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TorcetrapibCholesteryl ester transfer proteinIC 50 (nM)39N/AN/ADetails