期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 9, 页码 2456-2460出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.03.051
关键词
CETP; Cholesteryl ester transfer protein; HDL-C; Atherosclerosis
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. (c) 2009 Elsevier Ltd. All rights reserved.
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