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Design, Synthesis, and Evaluation of Fungicidal Activity of Novel Pyrazole‐Containing Strobilurin Derivatives †
Author(s) -
Hao Zesheng,
Wang Weibo,
Yu Bin,
Qi Xin,
Lv You,
Liu Xiaoyu,
Chen Haoyin,
Kalinina Tatiana A.,
Glukhareva Tatiana V.,
Fan Zhijin
Publication year - 2021
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.202000685
Subject(s) - azoxystrobin , strobilurin , fungicide , chemistry , gibberella zeae , sclerotinia sclerotiorum , carbendazim , bioassay , phytophthora infestans , pyrazole , stereochemistry , horticulture , biochemistry , biology , genetics , fusarium , gene
Main observation and conclusion In searching for novel fungicidal leads, a series of pyrazole‐containing strobilurins were rationally designed, synthesized and characterized. Bioassay indicated that compound I‐7 displayed excellent fungicidal activity against a broad spectrum of plant pathogens such as Gibberella zeae, Rhizoctonia cerealis, Sclerotinia sclerotiorum, Phytophthora infestans, Physalospora piricola and Pellicularia sasakii with EC 50 of 0.16, 0.02, 0.72, 0.07, 0.77 and 0.65 μg/mL, respectively, which were 3—10 times more potent than the positive control azoxystrobin against the corresponding pathogens. Moreover, like azoxystrobin and kresoxim methyl, I‐7, displayed excellent protective activity against P. sorghi . Molecular docking validated that I‐7 and azoxystrobin would share a similar binding mode with cytochrome bc 1 complex. This study demonstrates that I‐7 is a promising fungicidal candidate for further development.