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

[Display omitted] 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 preve...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2016-02, Vol.24 (3), p.354-361
Hauptverfasser: 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.
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Sprache:eng
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Zusammenfassung:[Display omitted] 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2015.07.064