Analogs of CPZEN-45, which is expected to be a promising new antituberculosis drug that overcomes the shortcomings of caprazamycins, were synthesized and their biological activities were evaluated. The biological activity of analogs 1-3, which converted the anilide portion, and analogs 4 and 5, focusing on the seven-membered ring, were lower than that of CPZEN-45. These results suggest that the inhibitory activity of CPZEN-45 against TagO, an ortholog of WecA, has a strict structural limitation, and it was hoped for elucidation of the mode of action of CPZEN-45 using structural biology in the future.

中文翻译：

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新型抗结核药物 CPZEN-45 类似物的合成及生物活性。

CPZEN-45的类似物被合成，有望成为一种有前途的新型抗结核药物，克服了卡扎霉素的缺点，并对其生物活性进行了评价。转化苯胺部分的类似物 1-3 以及集中在七元环上的类似物 4 和 5 的生物活性低于 CPZEN-45。这些结果表明CPZEN-45对WecA的直系同源物Tago的抑制活性具有严格的结构限制，未来有望利用结构生物学阐明CPZEN-45的作用方式。