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. 2009 May 1;19(9):2456-60.
doi: 10.1016/j.bmcl.2009.03.051. Epub 2009 Mar 18.

Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform

Thomas A Rano  1 , Ellen Sieber-McMaster, Patricia D Pelton, Maria Yang, Keith T Demarest, Gee-Hong Kuo
Affiliations

Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform

Thomas A Rano et al. Bioorg Med Chem Lett. .

Abstract

Tetrahydroquinoline A is a potent inhibitor of the cholesterol ester transfer protein (CETP), a target for the treatment of low HDL-C and atherosclerosis. Low HDL-C has been identified as a key risk factor for cardiovascular disease in addition to high LDL-C, the target of the statin drugs. Tetrahydroquinoline A inhibits partially purified CETP with an IC(50) of 39nM. The preparation of a series of potent inhibitors of CETP designed around a 1,2,3,4-tetrahydroquinoline platform will be discussed.

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