title: Discovery of oxathiapiprolin, a new oomycete fungicide that targets an oxysterol binding protein.
abstract: 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.
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA. Electronic address: robert.j.pasteris@dupont.com.
authors: Robert J
authors: RJ
authors: Pasteris
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: Mary Ann
authors: MA
authors: Hanagan
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: John J
authors: JJ
authors: Bisaha
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: Bruce L
authors: BL
authors: Finkelstein
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: Lisa E
authors: LE
authors: Hoffman
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: Vann
authors: V
authors: Gregory
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: John L
authors: JL
authors: Andreassi
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: James A
authors: JA
authors: Sweigard
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: Boris A
authors: BA
authors: Klyashchitsky
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: Yewande T
authors: YT
authors: Henry
authors: DuPont Crop Protection, Discovery Research, Stine-Haskell Research Center, PO Box 30, Newark, DE 19714, USA.
authors: Richard A
authors: RA
authors: Berger
mesh_terms: D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D006845:Hydrocarbons, Fluorinated / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009868:Oomycetes / Q000187:drug effects* / Q000378:metabolism*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011987:Receptors, Steroid / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000098825:Oxysterol Binding Proteins
chemical_list: D006845:Hydrocarbons, Fluorinated; D011720:Pyrazoles; D011987:Receptors, Steroid; D000098825:Oxysterol Binding Proteins; C000592431:oxathiapiprolin
keywords: Crop protection; Disease control; Oomycete fungicide; Oxathiapiprolin; Oxysterol binding protein