期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 24, 页码 6017-6021出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.09.077
关键词
CVT-4325; metabolic shift; fatty acid oxidation inhibitor
New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50 = 380 nM rat mitochondria) with favorable PK properties (F= 93%, t(1/2) = 13.6 h, dog). (C) 2004 Elsevier Ltd. All rights reserved.
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