Lamberth Clemens, Kessabi Fiona Murphy, Beaudegnies Renaud, Quaranta Laura, Trah Stephan, Berthon Guillaume, Cederbaum Fredrik, Knauf-Beiter Gertrud, Grasso Valeria, Bieri Stephane, Corran Andy, Thacker Urvashi
Syngenta Crop Protection AG, Research Chemistry, Schaffhauserstr. 101, CH-4332 Stein, Switzerland.
Syngenta Crop Protection AG, Research Chemistry, Schaffhauserstr. 101, CH-4332 Stein, Switzerland.
Bioorg Med Chem. 2014 Aug 1;22(15):3922-30. doi: 10.1016/j.bmc.2014.06.015. Epub 2014 Jun 17.
A novel class of experimental fungicides has been discovered, which consists of special quinolin-6-yloxyacetamides. They are highly active against important phytopathogens, such as Phytophthora infestans (potato and tomato late blight), Mycosphaerella graminicola (wheat leaf blotch) and Uncinula necator (grape powdery mildew). Their fungicidal activity is due to their ability to inhibit fungal tubulin polymerization, leading to microtubule destabilization. An efficient synthesis route has been worked out, which allows the diverse substitution of four identified key positions across the molecular scaffold.
已发现一类新型实验性杀菌剂,其由特殊的喹啉 - 6 - 基氧基乙酰胺组成。它们对重要的植物病原体具有高活性,如致病疫霉(马铃薯和番茄晚疫病)、小麦黄斑叶枯病菌(小麦叶斑病)和葡萄白粉病菌(葡萄白粉病)。它们的杀菌活性归因于其抑制真菌微管蛋白聚合的能力,从而导致微管不稳定。已制定出一条有效的合成路线,该路线允许在分子支架的四个已确定关键位置进行多样取代。