Synthesis and fungicidal activity of tubulin polymerisation promoters. Part 3: Imidazoles

被引：32

作者：

Lamberth, Clemens ^{[1
]}

Dumeunier, Raphael ^{[1
]}

Trah, Stephan ^{[1
]}

Wendeborn, Sebastian ^{[1
]}

Godwin, Jeremy ^{[1
]}

Schneiter, Peter ^{[1
]}

Corran, Andy ^{[2
]}

机构：

[1] Syngenta Crop Protect AG, Crop Protect Res, CH-4332 Stein, Switzerland

[2] Syngenta Ltd, Jealotts Hill Int Res Ctr, Bracknell RG42 6EY, Berks, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2013年 / 21卷 / 01期

关键词：

Tubulin; Imidazole; Heterocycle; Fungicide; Crop protection; CYCLOADDITION;

D O I：

10.1016/j.bmc.2012.10.052

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A novel class of experimental fungicides has been discovered, which consists of special tetrasubstituted midazoles. They are highly active against important phytopathogens, such as Botrytis cinerea (grey mould), Uncinula necator (grape powdery mildew), Mycosphaerella graminicola (wheat leaf blotch) and Alternaria solani (potato and tomato early blight). Their fungicidal efficacy is due to their ability to promote fungal tubulin polymerization, which leads to a disruption of microtubule dynamics. These imidazoles are five-membered ring analogs of similar substituted triazolopyrimidines and pyridazines with the same mode of action. A concise four-step synthesis route has been used to prepare them from commercially available starting materials. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：127 / 134

页数：8

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