Trifluoromethyloxadiazoles: inhibitors of histone deacetylases for control of Asian soybean rust.

Autor: Winter C; BASF SE, Agricultural Solutions, Ludwigshafen, Germany., Fehr M; BASF SE, Agricultural Solutions, Ludwigshafen, Germany., Craig IR; BASF SE, Digitalization in R&D, Ludwigshafen, Germany., Grammenos W; BASF SE, Agricultural Solutions, Ludwigshafen, Germany., Wiebe C; BASF SE, Agricultural Solutions, Ludwigshafen, Germany., Terteryan-Seiser V; BASF SE, Agricultural Solutions, Ludwigshafen, Germany., Rudolf G; BASF SE, Agricultural Solutions, Ludwigshafen, Germany., Mentzel T; BASF SE, Agricultural Solutions, Ludwigshafen, Germany., Quintero Palomar MA; BASF SE, Agricultural Solutions, Ludwigshafen, Germany.
Jazyk: angličtina
Zdroj: Pest management science [Pest Manag Sci] 2020 Oct; Vol. 76 (10), pp. 3357-3368. Date of Electronic Publication: 2020 May 22.
DOI: 10.1002/ps.5874
Abstrakt: Background: Trifluoromethyloxadiazoles (TFMOs) are selective inhibitors of class II histone deacetylases (HDACs). To date, class II HDACs have not been addressed as target enzymes by commercial fungicides.
Results: Antifungal testing of a broad variety of TFMOs against several important plant pathogens showed activity against only rusts, and especially Phakopsora pachyrhizi, the cause of Asian soybean rust. A structure-activity relationship was established, leading to highly active fungicides that inhibit fungal class II and HOS3-type HDACs of Aspergillus nidulans. Studies of the enzyme-inhibitor binding mode using protein structural information based on the crystal structure of human HDAC4 argue that TFMOs inhibit these enzymes only after undergoing hydration.
Conclusion: Fungal class II HDACs are potential target enzymes for the control of at least some biotrophic crop diseases, in particular Asian soybean rust. As with any novel mode-of-action, class II HDAC fungicides would offer the potential to control fungal isolates that show reduced sensitivity toward existing commercial fungicides.
(© 2020 Society of Chemical Industry.)
Databáze: MEDLINE
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