Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.

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Fernandez MC, Escribano A, Mateo AI, Parthasarathy S, Martin de la Nava EM, Wang X, Cockerham SL, Beyer TP, Schmidt RJ, Cao G, Zhang Y, Jones TM, Borel A, Sweetana SA, Cannady EA, Stephenson G, Frank S, Mantlo NB

Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.

Bioorg Med Chem Lett. 2012 May 1;22(9):3056-62. doi: 10.1016/j.bmcl.2012.03.075. Epub 2012 Mar 28.

PubMed ID

22497761 [ View in PubMed

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Abstract

This Letter describes the discovery and SAR optimization of 1,5-tetrahydronaphthyridines, a new class of potent CETP inhibitors. The effort led to the identification of 21b and 21d with in vitro human plasma CETP inhibitory activity in the nanomolar range (IC(50)=23 and 22nM, respectively). Both 21b and 21d exhibited robust HDL-c increase in hCETP/hApoA1 dual heterozygous mice model.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Torcetrapib	Cholesteryl ester transfer protein	IC 50 (nM)	39	N/A	N/A	Details