Synthesis, Fungicidal Activity, and Structure Activity Relationship of [beta]-Acylaminocycloalkylsulfonamides against Botrytis cinerea

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 1 H NMR, 13 C NMR, IR, MS, elemental analysis and X-ray single crystal diffra...

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Published inScientific reports Vol. 7; p. 42096
Main Authors Liu, Chun-hui, Chen, Xiao-yuan, Qin, Pei-wen, Qi, Zhi-qiu, Ji, Ming-shan, Liu, Xing-yu, Babu, P Vijaya, Li, Xing-hai, Cui, Zi-ning
Format Journal Article
LanguageEnglish
Published London Nature Publishing Group 01.02.2017
Subjects
Agrochemicals
Antifungal agents
Bioassays
Diffraction
Disease control
Fungicidal activity
Fungicides
Hydrocarbons
Laboratories
NMR
Nuclear magnetic resonance
Pathogens
Pesticides
Plant diseases
Procymidone
Single crystals
Sulfonamides
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Summary: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 1 H NMR, 13 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 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.
ISSN:2045-2322
DOI:10.1038/srep42096