Design, Synthesis, and Antifungal Activity of 16,17-Dihydroheronamide C and <i>ent</i>-Heronamide C
Design, Synthesis, and Antifungal Activity of 16,17-Dihydroheronamide C and <i>ent</i>-Heronamide C
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16,17-二氢海洛酰胺 C 和 <i>ent</i>-Heronamide C 的设计、合成和抗真菌活性
DOI：
10.1021/acs.joc.1c01761
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发表时间：
2021
期刊：
影响因子：
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通讯作者：
Kakeya Hideaki
中科院分区：
文献类型：
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作者：
Kanoh Naoki;Terashima Ryusei;Nishiyama Hiromichi;Terajima Yuta;Nagasawa Shota;Sasano Yusuke;Iwabuchi Yoshiharu;Saito Hiroaki;Egoshi Syusuke;Dodo Kosuke;Sodeoka Mikiko;Pan Chengqian;Ikeuchi Yoshinobu;Nishimura Shinichi;Kakeya Hideaki
设计了16，17-二氢香草酰胺C(8)和二氢香草酰胺C(ENT-1)作为探针，用于香草酰胺C(1)的作用模式分析。这些分子是利用前一篇论文中开发的高度模块化的策略合成的。对这些化合物的抗真菌活性的评价表明，C16-C17双键对于草酰胺C的抗真菌活性非常重要，并且草酰胺C(1)与细胞膜成分之间存在手性识别。
16,17-Dihydroheronamide C (8) andent-heronamide C (ent-1) were designed as probes for the mode-of-action analysis of heronamide C (1). These molecules were synthesized by utilizing a highly modular strategy developed in the preceding paper. The evaluation of the antifungal activity of these compounds revealed the exceptional importance of the C16–C17 double bond for the antifungal activity of heronamide C and the existence of chiral recognition between heronamide C (1) and cell membrane components.