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5-(羟基亚氨基)-4-甲氧基-2-(新戊酰亚氨基)噻唑烷-3-乙酰胺,一种具有强效杀血吸虫特性的还原型硝基杂环衍生物。

5-(Hydroxyimino)-4-methoxy-2-(pivaloylimino)thiazolidine-3 -acetamide, a reduced nitroheterocyclic derivative with potent schistosomicidal properties.

作者信息

Islip P J, Bogunović-Batchelor M V

出版信息

Experientia. 1985 Oct 15;41(10):1353-4. doi: 10.1007/BF01952092.

Abstract

The synthesis and antischistosome properties of 5-(hydroxyimino)-4-methoxy-2-(pivaloylimino)thiazolidine-3- acetamide (1) are described. The compound was prepared by reduction of the nitrothiazoline (2) with stannous chloride in methanol, and represents the first example of a reduced nitroheterocyclic compound showing potent schistosomicidal properties. The possible relationship of compounds such as 1 to the as yet unidentified reduced active but toxic entities formed in vivo from nitroheterocyclics like metronidazole is discussed.

摘要

描述了5-(羟基亚氨基)-4-甲氧基-2-(新戊酰亚氨基)噻唑烷-3-乙酰胺(1)的合成及其抗血吸虫特性。该化合物是通过在甲醇中用氯化亚锡还原硝基噻唑啉(2)制备的,它是显示出强效杀血吸虫特性的还原硝基杂环化合物的首个实例。讨论了化合物1等与甲硝唑等硝基杂环化合物在体内形成的尚未明确的还原活性但有毒的实体之间可能的关系。

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