Discovery of oxathiapiprolin, a new oomycete fungicide that targets an oxysterol binding protein
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- 作者：Robert J. Pasteris ; robert.j.pasteris@dupont.com" class="auth_mail" title="E-mail the corresponding author ; 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
- 关键词：IAQLCKZJGNTRDO-UHFFFAOYSA-N
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：1 February 2016
- 年：2016
- 卷：24
- 期：3
- 页码：354-361
- 全文大小：891 K
文摘
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.