Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2015-07-31 , DOI: 10.1016/j.bmc.2015.07.064 Robert J. Pasteris , Mary Ann Hanagan , John J. Bisaha , Bruce L. Finkelstein , Lisa E. Hoffman , Vann Gregory , John L. Andreassi , James A. Sweigard , Boris A. Klyashchitsky , Yewande T. Henry , Richard A. Berger
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.
中文翻译:
发现氧杂泛醇,一种靶向氧固醇结合蛋白的新型卵菌杀菌剂
Oxathiapiprolin是一类新的哌啶基噻唑异恶唑啉类杀菌剂的第一个成员,对由卵菌病原体引起的植物病害具有出色的活性。它通过抑制新型真菌靶标(氧固醇结合蛋白)发挥作用,从而对葡萄,土豆和蔬菜等关键疾病具有出色的预防,治疗和残留功效。Oxathiapiprolin作为DuPont™Zorvec™疾病控制产品正在全球范围内开发,预计于2015年首次注册和销售。其中介绍了其发现,合成,优化和生物学功效。