Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform |
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Authors: | Thomas A Rano Ellen Sieber-McMaster Patricia D Pelton Maria Yang Keith T Demarest Gee-Hong Kuo |
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Institution: | Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Metabolic Disorders Team, 1000 Route 202, P.O. Box 300, Raritan, NJ 08869, United States |
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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 IC50 of 39 nM. 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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