壬基3-酰基二硫代氨基甲酸盐及相关化合物的解偶联活性的合成与构效关系

Synthesis and structure--activity relationship of nonyl 3-acyldithiocarbazates and related compounds for uncoupling activities.

作者信息

Uda M, Toyooka K, Horie K, Shibuya M, Kubota S, Terada H

出版信息

J Med Chem. 1982 May;25(5):557-60. doi: 10.1021/jm00347a015.

Abstract

Various nonyl 3-substituted-dithiocarbazates, methyl and dimethyl derivatives of nonyl 3-benzoyldithiocarbazate, nonyl 2-substituted-dithiocarbamates, and benzaldehyde nonyldithiocarbohydrazone were synthesized and their uncoupling activities of oxidative phosphorylation in mitochondria were examined. The results indicate that the presence of the thiocarbamoyl structure with the potential SH group is a requisite for uncoupling activity. The presence of a C=O group and a hydrophobic aromatic ring significantly increases the uncoupling activity.

摘要

合成了各种壬基3-取代二硫代氨基甲酸盐、壬基3-苯甲酰基二硫代氨基甲酸盐的甲基和二甲基衍生物、壬基2-取代二硫代氨基甲酸盐以及苯甲醛壬基二硫代碳酰腙，并检测了它们在线粒体中氧化磷酸化的解偶联活性。结果表明，具有潜在巯基的硫代甲酰结构的存在是解偶联活性的必要条件。羰基和疏水芳环的存在显著增加了解偶联活性。