10591-84-1Relevant articles and documents
Development of disulfide-derived fructose-1,6-bisphosphatase (FBPase) covalent inhibitors for the treatment of type 2 diabetes
Xu, Yi-xiang,Huang, Yun-yuan,Song, Rong-rong,Ren, Yan-liang,Chen, Xin,Zhang, Chao,Mao, Fei,Li, Xiao-kang,Zhu, Jin,Ni, Shuai-shuai,Wan, Jian,Li, Jian
, (2020)
Fructose-1,6-bisphosphatase (FBPase), as a key rate-limiting enzyme in the gluconeogenesis (GNG) pathway, represents a practical therapeutic strategy for type 2 diabetes (T2D). Our previous work first identified cysteine residue 128 (C128) was an important allosteric site in the structure of FBPase, while pharmacologically targeting C128 attenuated the catalytic ability of FBPase. Herein, ten approved cysteine covalent drugs were selected for exploring FBPase inhibitory activities, and the alcohol deterrent disulfiram displayed superior inhibitory efficacy among those drugs. Based on the structure of lead compound disulfiram, 58 disulfide-derived compounds were designed and synthesized for investigating FBPase inhibitory activities. Optimal compound 3a exhibited significant FBPase inhibition and glucose-lowering efficacy in vitro and in vivo. Furthermore, 3a covalently modified the C128 site, and then regulated the N125–S124–S123 allosteric pathway of FBPase in mechanism. In summary, 3a has the potential to be a novel FBPase inhibitor for T2D therapy.
Continuous-flow step-economical synthesis of thiuram disulfidesviavisible-light photocatalytic aerobic oxidation
Xu, Hao-Xing,Zhao, Ze-Run,Patehebieke, Yeersen,Chen, Qian-Qian,Fu, Shun-Guo,Chang, Shuai-Jun,Zhang, Xu-Xu,Zhang, Zhi-Liang,Wang, Xiao
, p. 1280 - 1285 (2021)
A continuous-flow photocatalytic synthesis of the industrially important thiuram disulfides has been developed, utilizing O2as the oxidant and Eosin Y as the photoredox catalyst. This highly atom- and step-economical method features much reduced reaction time as well as excellent product yield and purity, making it a sustainable and potentially scalable process for industrial production.
Thiuram disulfide compound and synthesis process thereof
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Paragraph 0044-0048, (2019/03/25)
The invention belongs to the field of rubber additives and particularly relates to a thiuram disulfide compound and a synthesis process thereof. The synthesis process comprises the following steps: (1) mixing secondary amine with alkaline liquid, then dropwise adding carbon disulfide, wherein the molar ratio of the secondary amine to the alkaline liquid to the carbon disulfide is 1 to (1-2) to (1-2), and reacting at the temperature of 30-60 DEG C to obtain a sodium dithioformate intermediate; (2) mixing and stirring the sodium dithioformate intermediate obtained in the step (1), dimethylsulfoxide and a dispersant, dropwise adding a strong acid catalyst and reacting at the temperature of 30-80 DEG C, wherein the molar ratio of the sodium dithioformate intermediate to the dimethylsulfoxide to the strong acid catalyst is 2 to (1-1.8) to (2-4), and the molar amount of the catalyst is metered by hydrogen ions; and generating a target product. The product yield of the reaction can reach 95%or above; through HPLC test of the product, the purity can reach up to 96%.