Author/Authors :
Elfatih Elzein، نويسنده , , Kevin Shenk، نويسنده , , Prabha Ibrahim، نويسنده , , Tim Marquart، نويسنده , , Suresh Kerwar، نويسنده , , Stephanie Meyer، نويسنده , , Hiba Ahmed، نويسنده , , Dewan Zeng، نويسنده , , Nancy Chu، نويسنده , , Daniel Soohoo، نويسنده , , Shirley Wong، نويسنده , , Kwan-Leung Chan MD FRCPC، نويسنده , , Jeff Zablocki، نويسنده ,
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, IC50=70 nM; 25, IC50=23 nM).
