期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 20, 页码 5872-5876出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.077
关键词
Carboxylase; ACC; ACC inhibitors; Biphenyl; 3-Phenyl pyridine
We report the synthesis and enzymatic evaluation of potent inhibitors of acetyl-CoA carboxylases (ACCs) containing biphenyl or 3-phenyl pyridine cores. These compounds inhibit both ACC1 and ACC2, or are moderately selective for either enzyme, depending on side chain substitution. Typical activities of the most potent compounds in this class are in the low double-digit to single-digit nanomolar range in in vitro assays using human ACC1 and ACC2 enzymes. (C) 2009 Elsevier Ltd. All rights reserved.
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