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一些具有抗寄生虫活性的硝基呋喃噻唑的处置与代谢

Disposition and metabolism of some nitrofurylthiazoles possessing antiparasitic activity.

作者信息

Chatfield D H

出版信息

Xenobiotica. 1976 Aug;6(8):509-20. doi: 10.3109/00498257609151663.

Abstract
  1. The absorption, distribution and excretion of two 35S-labelled nitrofurylthiazole analogues have been investigated in rats and mice. The compounds are not well absorbed. Higher plasma and tissue levels are reached when more water-soluble analogues are administered. 2. Metabolic transformations of these two compounds and other membranes of the series include reduction of the nitro group, degradation of the furan ring and oxidation of the terminal alicyclic and aliphatic functions. 3. Metabolic cleavage of a morpholine ring to form an hydroxy-acid has been demonstrated for one member of the series.
摘要
  1. 对两种35S标记的硝基呋喃噻唑类似物在大鼠和小鼠体内的吸收、分布及排泄情况进行了研究。这些化合物吸收不佳。给予水溶性更高的类似物时,血浆和组织中的水平会更高。2. 这两种化合物及该系列的其他成员的代谢转化包括硝基的还原、呋喃环的降解以及末端脂环族和脂肪族官能团的氧化。3. 已证实该系列中的一个成员会发生吗啉环的代谢裂解以形成羟基酸。

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