Terada H, Uda M, Kametani F, Kubota S
Biochim Biophys Acta. 1978 Nov 9;504(2):237-47. doi: 10.1016/0005-2728(78)90172-x.
A structure-activity relationship study on the uncoupling of alkyl acyldithiocarbazates was carried out. Greater activity was observed with increasing alkyl chain length, the optimum being C9. A further increase in alkyl chain length caused a decrease in the activity. Thione-thiol tautomeric forms with a dissociable proton were dound to be of primary importance for the uncoupling and the role of the acyl group was auxiliary. The reactivity of the SH group of alkyl acyldithiocarbazates with an SH-reagent was very low. These compounds facilitated the valinomycin-induced swelling of non-respiring mitochondria and non-sonicated lecithin liposomes in isotonic potassium acetate solution.
开展了关于烷基酰基二硫代卡巴腙解偶联作用的构效关系研究。观察到随着烷基链长度增加活性增强，最佳长度为C9。烷基链长度进一步增加导致活性降低。发现具有可解离质子的硫酮-硫醇互变异构形式对于解偶联至关重要，而酰基的作用是辅助性的。烷基酰基二硫代卡巴腙的SH基团与SH试剂的反应性非常低。这些化合物在等渗醋酸钾溶液中促进了缬氨霉素诱导的非呼吸性线粒体和未超声处理的卵磷脂脂质体肿胀。
