Synthesis and fungicidal activity of tubulin polymerisation promoters. Part 2: Pyridazines
Synthesis and fungicidal activity of tubulin polymerisation promoters. Part 2: Pyridazines
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DOI：
10.1016/j.bmc.2012.03.035
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发表时间：
2012-05-01
影响因子：
3.5
通讯作者：
Schneiter, Peter
中科院分区：
文献类型：
--
作者：
Lamberth, Clemens;Trah, Stephan;Schneiter, Peter
特殊的四取代哒嗪是有效的杀菌剂，可促进微管蛋白聚合，从而破坏真菌中的微管动力学。它们是类似取代的三唑并嘧啶和吡啶并吡嗪的单环类似物，具有相同的作用方式。评估了这些哒嗪类化合物对植物病原体灰霉病（灰霉病）、禾生球腔菌（小麦叶斑病）和黑斑病（马铃薯和番茄早疫病）的杀菌活性。结构-活性关系研究揭示了紧邻两个环氮原子的甲基和氯取代基以及其他两个哒嗪位置的两个芳基或杂芳基的重要性。 (C) 2012 Elsevier Ltd. 保留所有权利。
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 graminicola (wheat leaf blotch) and Alternaria solani (potato and tomato early blight). Structure-activity relationship studies revealed the importance of a methyl and a chlorine substituent next to both ring nitrogen atoms and two aryl or heteroaryl groups in the other two pyridazine positions. (C) 2012 Elsevier Ltd. All rights reserved.