Kubota S, Uda M, Mori Y, Kametani F, Terada H
J Med Chem. 1978 Jun;21(6):591-4. doi: 10.1021/jm00204a018.
A series of alkyl dithiocarbazates, alkyl 3-picolinoyldithiocarbazates, alkyl 3-nicotinoyldithiocarbazates, alkyl 3-isonicotinoyldithiocarbazates, and alkyl 3-picolinoyl-2-methyldithiocarbazates was prepared. These alkyl pyridinecarbonyldithiocarbazates were shown to be uncouplers of oxidative phosphorylation in mitochondria. The finding that uncoupling activity increased with increase in the length of the alkyl chains of the compounds indicates that hydrophobicity influences the activity. The nonyl derivatives had the highest activity. The results also suggested that a dissociable acidic proton is necessary for the uncoupling activity.
制备了一系列烷基二硫代氨基甲酸盐、烷基3-吡啶甲酰基二硫代氨基甲酸盐、烷基3-烟酰基二硫代氨基甲酸盐、烷基3-异烟酰基二硫代氨基甲酸盐和烷基3-吡啶甲酰基-2-甲基二硫代氨基甲酸盐。这些烷基吡啶羰基二硫代氨基甲酸盐被证明是线粒体氧化磷酸化的解偶联剂。化合物的解偶联活性随烷基链长度增加而增强这一发现表明，疏水性会影响活性。壬基衍生物具有最高活性。结果还表明，可解离的酸性质子对于解偶联活性是必需的。
