- Novel inhibitors of fatty acid oxidation as potential metabolic modulators.
Novel inhibitors of fatty acid oxidation as potential metabolic modulators.
Bioorganic & medicinal chemistry letters (2004-03-12)
Elfatih Elzein, Kevin Shenk, Prabha Ibrahim, Tim Marquart, Suresh Kerwar, Stephanie Meyer, Hiba Ahmed, Dewan Zeng, Nancy Chu, Daniel Soohoo, Shirley Wong, Kwan Leung, Jeff Zablocki
PMID15013004
ABSTRACT
We describe the synthesis of novel inhibitors of fatty acid oxidation as potential metabolic modulators for the treatment of stable angina. Replacement of the 2H-benzo[d]1,3-dioxolene ring system in our initial lead 3 with different benzthiazoles, benzoxazoles and introducing small alkyl substituents into the piperazine ring resulted in analogues with enhanced inhibitory activity against 1-(14)[C]-palmitoyl-CoA oxidation in isolated rat heart mitochondria (6, IC(50)=70 nM; 25, IC(50)=23 nM).
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