Undefeated—Changing the phenamacril scaffold is not enough to beat resistant Fusarium
Undefeated—Changing the phenamacril scaffold is not enough to beat resistant Fusarium
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DOI：
10.1371/journal.pone.0235568
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发表时间：
2020-06
期刊：
影响因子：
3.7
通讯作者：
R. Wollenberg;S. S. Donau-S.;M. Taft;Z. Balázs;Sven H. Giese;C. Thiel;J. L. Sørensen;T. T. Nielsen-T.;H. Giese;D. Manstein;R. Wimmer;T. E. Sondergaard
中科院分区：
文献类型：
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作者：
R. Wollenberg;S. S. Donau-S.;M. Taft;Z. Balázs;Sven H. Giese;C. Thiel;J. L. Sørensen;T. T. Nielsen-T.;H. Giese;D. Manstein;R. Wimmer;T. E. Sondergaard
属于镰刀菌属的丝状真菌是一种臭名昭著的植物病原菌，可以侵染、危害和污染多种重要的农作物。苯那普利是一类新型的单部位作用氰基丙烯酸酯类杀菌剂中的第一个成员，已被证明对镰刀菌属的重要成员具有高度的有效性。然而，最近出现的表现出质量抗性的田间抗性菌株对苯那普利的继续使用构成了主要障碍。在这项研究中，我们合成了基于苯那普利支架的新型氰基丙烯酸酯化合物，以测试它们对野生型镰刀菌和苯那普利耐药菌株的生长抑制潜力。我们的发现表明，对苯那普利支架的大多数化学修饰与几乎完全失去杀菌活性和体外抑制肌球蛋白运动域ATPase活性有关。
Filamentous fungi belonging to the genus Fusarium are notorious plant-pathogens that infect, damage and contaminate a wide variety of important crops. Phenamacril is the first member of a novel class of single-site acting cyanoacrylate fungicides which has proven highly effective against important members of the genus Fusarium. However, the recent emergence of field-resistant strains exhibiting qualitative resistance poses a major obstacle for the continued use of phenamacril. In this study, we synthesized novel cyanoacrylate compounds based on the phenamacril-scaffold to test their growth-inhibitory potential against wild-type Fusarium and phenamacril-resistant strains. Our findings show that most chemical modifications to the phenamacril-scaffold are associated with almost complete loss of fungicidal activity and in vitro inhibition of myosin motor domain ATPase activity.