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Updated: Aug 29, 2026

Determination of Fatty Acid Oxidation and Lipogenesis in Mouse Primary Hepatocytes
Published on: August 27, 2015
New fatty acid oxidation inhibitors with increased potency lacking adverse metabolic and electrophysiological
Dmitry O Koltun1, Timothy A Marquart, Kevin D Shenk
1Department of Bioorganic Chemistry, 3172 Porter Dr., Palo Alto, CA 94304, USA. dmitry.koltun@cvt.com
Abstract:
New inhibitors of palmitoylCoA oxidation were synthesized based on a structurally novel lead, CVT-3501 (1). Investigation of structure-activity relationships was conducted with respect to potency of inhibition of cardiac mitochondrial palmitoylCoA oxidation and metabolic stability. Potent and metabolically stable analogues 33, 42, and 43 were evaluated in vitro for cytochrome P450 inhibition and potentially adverse electrophysiological effects. Compound 33 was also found to have favorable pharmacokinetic properties in rat.
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