期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 9, 页码 3056-3062出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.03.075
关键词
CETP inhibitor; HDL-c; CVD; 1,5-Tetrahydronaphthyridines
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 (IC50 = 23 and 22 nM, respectively). Both 21b and 21d exhibited robust HDL-c increase in hCETP/hApoA1 dual heterozygous mice model. (C) 2012 Elsevier Ltd. All rights reserved.
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