Synthesis and fungicidal activity of tubulin polymerisation promoters. Part 2: Pyridazines
作者:Clemens Lamberth、Stephan Trah、Sebastian Wendeborn、Raphael Dumeunier、Mikael Courbot、Jeremy Godwin、Peter Schneiter
DOI:10.1016/j.bmc.2012.03.035
日期:2012.5
Special tetrasubstituted pyridazines are potent fungicides by promoting the tubulin polymerisation, hereby disrupting the microtubule dynamics in the fungus. They are monocyclic analogs of similar substituted triazolopyrimidines and pyridopyrazines with the same mode of action. The fungicidal activity of these pyridazines was evaluated against the plant pathogens Botrytis cinerea (grey mould), Mycosphaerella
特殊的四取代哒嗪是有效的杀真菌剂,可促进微管蛋白聚合,从而破坏真菌中的微管动力学。它们是具有相同作用方式的类似取代的三唑并嘧啶和吡啶并吡嗪的单环类似物。评估了这些哒嗪对植物病原体灰葡萄孢(Botrytis cinerea),灰色霉菌(Mycosphaerella graminicola)(小麦叶片斑点)和链格孢链霉菌(Alternaria solani)(马铃薯和番茄早疫病)的杀真菌活性。结构-活性关系研究表明,在环氮原子和其他两个哒嗪位置上的两个芳基或杂芳基旁边,都应有一个甲基和一个氯取代基,这一点很重要。