Arsinothricin [AST (1)], a new broad-spectrum organoarsenical antibiotic, is a nonproteinogenic analogue of glutamate that effectively inhibits glutamine synthetase. We report the chemical synthesis of an intermediate in the pathway to 1, hydroxyarsinothricin [AST-OH (2)], which can be converted to 1 by enzymatic methylation catalyzed by the ArsM As(III) S-adenosylmethionine methyltransferase. This is the first report of semisynthesis of 1, providing a source of this novel antibiotic that will be required for future clinical trials.

中文翻译：

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有机砷抗生素 Arsinothricin 的半合成。

Arsinothricin [AST ( 1 )] 是一种新的广谱有机砷抗生素，是一种非蛋白原性谷氨酸类似物，可有效抑制谷氨酰胺合成酶。我们报告了到1的途径中的中间体的化学合成，羟基胼胝素[AST-OH ( 2 )]，它可以通过由 ArsM As(III) S-腺苷甲硫氨酸甲基转移酶催化的酶促甲基化转化为1。这是半合成的第一次报告1，提供了将需要将来的临床试验此新型抗生素的来源。