Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373097 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
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.
Graphical abstractWe report potent biphenyl- and 3-phenyl pyridine-based inhibitors of human acetyl-CoA carboxylase (ACC) enzymes 1 and 2.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Tasir S. Haque, Ningning Liang, Rajasree Golla, Ramakrishna Seethala, Zhengping Ma, William R. Ewing, Christopher B. Cooper, Mary Ann Pelleymounter, Michael A. Poss, Dong Cheng,