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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Nakaoka M, Hakusui H, Takegoshi T

Research Institute, Daiichi Seiyaku Co., Ltd., Tokyo, Japan.

Xenobiotica. 1989 Feb;19(2):209-16. doi: 10.3109/00498258909034693.

The metabolism of malotilate, possessing a 1,3-dithiole ring, was studied in rats. A major biliary metabolite of malotilate was isolated and determined to be a thio-glucuronide of the dithiol formed by ring-opening, namely, 1-mercapto-2,2-di(isopropoxycarbonyl)-ethenyl 1-thio-beta-D-glucosiduronic acid. The structure was elucidated by proton-n.m.r., 13C-n.m.r. and high-resolution mass spectrometry. 2. The thio-glucuronide was completely hydrolysed by beta-glucuronidase. This enzymic reaction was inhibited by saccharo-1,4-lactone.

在大鼠体内研究了具有1,3 - 二硫杂环戊烯环的马洛替酯的代谢情况。分离出了马洛替酯的一种主要胆汁代谢物，经测定它是由开环形成的二硫醇的硫代葡糖醛酸，即1 - 巯基 - 2,2 - 二（异丙氧基羰基） - 乙烯基1 - 硫代 - β - D - 葡糖苷醛酸。通过质子核磁共振、碳 - 13核磁共振和高分辨率质谱对其结构进行了阐明。2. 硫代葡糖醛酸可被β - 葡糖醛酸酶完全水解。该酶促反应受到1,4 - 内酯的抑制。

Nakaoka M, Hakusui H, Takegoshi T

Research Institute, Daiichi Seiyaku Co., Ltd., Tokyo, Japan.

Xenobiotica. 1989 Feb;19(2):209-16. doi: 10.3109/00498258909034693.

The metabolism of malotilate, possessing a 1,3-dithiole ring, was studied in rats. A major biliary metabolite of malotilate was isolated and determined to be a thio-glucuronide of the dithiol formed by ring-opening, namely, 1-mercapto-2,2-di(isopropoxycarbonyl)-ethenyl 1-thio-beta-D-glucosiduronic acid. The structure was elucidated by proton-n.m.r., 13C-n.m.r. and high-resolution mass spectrometry. 2. The thio-glucuronide was completely hydrolysed by beta-glucuronidase. This enzymic reaction was inhibited by saccharo-1,4-lactone.

在大鼠体内研究了具有1,3 - 二硫杂环戊烯环的马洛替酯的代谢情况。分离出了马洛替酯的一种主要胆汁代谢物，经测定它是由开环形成的二硫醇的硫代葡糖醛酸，即1 - 巯基 - 2,2 - 二（异丙氧基羰基） - 乙烯基1 - 硫代 - β - D - 葡糖苷醛酸。通过质子核磁共振、碳 - 13核磁共振和高分辨率质谱对其结构进行了阐明。2. 硫代葡糖醛酸可被β - 葡糖醛酸酶完全水解。该酶促反应受到1,4 - 内酯的抑制。