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

  作者 LAMBERTH CLEMENS; DUMEUNIER RAPHAEL; TRAH STEPHAN; WENDEBORN SEBASTIAN; GODWIN JEREMY; SCHNEITER PETER; CORRAN ANDY  
  选自 期刊  Bioorganic & Medicinal Chemistry;  卷期  2013年21-1;  页码  127-134  
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[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.

 
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