发现氧化噻唑啉，一种靶向氧化甾醇结合蛋白的新型卵菌纲杀菌剂。
Discovery of oxathiapiprolin, a new oomycete fungicide that targets an oxysterol binding protein.
作者信息
Pasteris Robert J, Hanagan Mary Ann, Bisaha John J, Finkelstein Bruce L, Hoffman Lisa E, Gregory Vann, Andreassi John L, Sweigard James A, Klyashchitsky Boris A, Henry Yewande T, Berger Richard A
机构信息
DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
出版信息
Bioorg Med Chem. 2016 Feb 1;24(3):354-61. doi: 10.1016/j.bmc.2015.07.064. Epub 2015 Jul 31.
Oxathiapiprolin is the first member of a new class of piperidinyl thiazole isoxazoline fungicides with exceptional activity against plant diseases caused by oomycete pathogens. It acts via inhibition of a novel fungal target-an oxysterol binding protein-resulting in excellent preventative, curative and residual efficacy against key diseases of grapes, potatoes and vegetables. Oxathiapiprolin is being developed globally as DuPont™ Zorvec™ disease control with first registration and sales anticipated in 2015. The discovery, synthesis, optimization and biological efficacy are presented.
恶唑菌酰胺是新型哌啶基噻唑异恶唑啉类杀菌剂的首个成员，对卵菌病原体引起的植物病害具有卓越活性。它通过抑制一种新型真菌靶点——氧化甾醇结合蛋白发挥作用，从而对葡萄、马铃薯和蔬菜的主要病害具有出色的预防、治疗和残留防效。恶唑菌酰胺正在全球范围内作为杜邦™ 唑菌胺酯™ 病害防治剂进行开发，预计2015年首次登记并上市销售。本文介绍了其发现、合成、优化及生物活性。
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