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Bioorg Med Chem Lett. 2004 Jan 19;14(2):549-52.

New fatty acid oxidation inhibitors with increased potency lacking adverse metabolic and electrophysiological properties.

Author information

1
Department 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.

PMID:
14698201
DOI:
10.1016/j.bmcl.2003.09.093
[Indexed for MEDLINE]

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