化学
哌嗪
β氧化
IC50型
戒指(化学)
立体化学
脂肪酸
铅化合物
烷基
代谢途径
抑制性突触后电位
组合化学
生物化学
体外
新陈代谢
有机化学
生物
神经科学
作者
Elfatih Elzein,Kevin D. Shenk,Prabha Ibrahim,Tim Marquart,S.S. Kerwar,Steven De Meyer,Hiba Ahmed,Dewan Zeng,Nancy Chu,Daniel Soohoo,Shirley M. E. Wong,Kwan Leung,Jeff Zablocki
标识
DOI:10.1016/j.bmcl.2003.11.065
摘要
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).
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