Discovery of oxathiapiprolin, a new oomycete fungicide that targets an oxysterol binding protein

摘要

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 (TM) Zorvec (TM) disease control with first registration and sales anticipated in 2015. The discovery, synthesis, optimization and biological efficacy are presented. (C) 2015 Elsevier Ltd. All rights reserved.