Synthesis and biological activity of analogs of CPZEN-45, a novel antituberculosis drug
Synthesis and biological activity of analogs of CPZEN-45, a novel antituberculosis drug
复制标题
DOI：
10.1038/s41429-019-0225-5
复制
发表时间：
2019-12-01
影响因子：
3.3
通讯作者：
Igarashi, Masayuki
中科院分区：
文献类型：
--
作者：
Ishizaki, Yoshimasa;Takahashi, Yoshiaki;Igarashi, Masayuki
CPZEN-45是一种有望克服Caprazamycins缺点的新型抗结核药物。本文合成了CPZEN-45类似物，并对其生物活性进行了评价。转化苯胺部分的类似物1-3和集中于七元环的类似物4和5的生物活性低于CPZEN-45的生物活性。这些结果表明，CPZEN-45对TagO（WecA的直系同源物）的抑制活性具有严格的结构限制，并且希望将来使用结构生物学来阐明CPZEN-45的作用方式。
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.