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Synthesis, Fungicidal Activity, and Structure Activity Relationship of ?-Acylaminocycloalkylsulfonamides against Botrytis cinerea.


ABSTRACT: In order to discover new antifungal agrochemicals that could have highly active and novel motifs, thirty-six new 2-acylaminocycloalkylsulfonamides (IV) were synthesized. Their structures were characterized and confirmed by 1H NMR, 13C NMR, IR, MS, elemental analysis and X-ray single crystal diffraction. In vitro and in vivo activities against various Botrytis cinerea strains were evaluated. Bioassay results revealed that most of the title compounds exhibited excellent in vitro fungicidal activity, in which compound IV-26 showed the highest activity against sensitive, low-resistant, moderate-resistant and high-resistant strains of B. cinerea compared with the positive fungicide procymidone. Meanwhile in vivo fungicidal activity of compound IV-31 was better than the commercial fungicides procymidone and chesulfamide in greenhouse trial. The structure activity relationship (SAR) was also discussed and the results were of importance to the structural optimization and development of more potent sulfonamides antifungal agents.

SUBMITTER: Liu CH 

PROVIDER: S-EPMC5296765 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature

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Synthesis, Fungicidal Activity, and Structure Activity Relationship of β-Acylaminocycloalkylsulfonamides against Botrytis cinerea.

Liu Chun-Hui CH   Chen Xiao-Yuan XY   Qin Pei-Wen PW   Qi Zhi-Qiu ZQ   Ji Ming-Shan MS   Liu Xing-Yu XY   Babu P Vijaya PV   Li Xing-Hai XH   Cui Zi-Ning ZN  

Scientific reports 20170208


In order to discover new antifungal agrochemicals that could have highly active and novel motifs, thirty-six new 2-acylaminocycloalkylsulfonamides (IV) were synthesized. Their structures were characterized and confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR, IR, MS, elemental analysis and X-ray single crystal diffraction. In vitro and in vivo activities against various Botrytis cinerea strains were evaluated. Bioassay results revealed that most of the title compounds exhibited excellent in vi  ...[more]

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