农药学学报Issue(1)：28-36,9.DOI:10.16801/j.issn.1008-7303.2016.0003
2-氧代-2-苯基乙磺酰胺化合物组合合成与杀菌活性研究
Combined synthesis and fungicidal activity evaluation of the 2-oxo-2-phenyl ethyl sulfonamide derivatives
摘要
Abstract
In order to rapidly prepare novel lead compounds of fungicides, the method that involved both the combinatorial chemistry and the conventional synthesis was used. The fungicidal activity againstBotrytis cinerea of the N-substituted-2-oxo-2-phenyl ethyl sulfonamide derivatives were investigated. Firstly, 2-oxo-2-phenyl ethyl sulfonyl chloride was prepared by the sulfonation and chlorination of acetophenone. Then 33 combinatorial libraries, which contained 105 compounds, were synthesized by the reaction of 2-oxo-2-phenyl ethyl sulfonyl chloride respectly with aniline, benzylamine or alkyl amine combination library. The yields ranged from 60% to 90% and the purity was 70% - 95%. Twenty-nine compounds were synthesized in parallel with 10 active libraries, within which 10 active compounds were purified and identified.In vitro and in vivo, all combination libraries and compounds were screened byBotrytis cinerea. Finally, the high activity lead compound was quickly determined, which lay the foundation for further structural optimization.关键词
乙磺酰胺/组合化学/灰霉病菌/杀菌活性/构效关系Key words
ethyl sulfonamide/combinatorial chemistry/Botrytis cinerea/fungicidal activity/structure-activity relationship分类
化学化工引用本文复制引用
李兴海,芮朋,潘强,陈小员,祁之秋,纪明山..2-氧代-2-苯基乙磺酰胺化合物组合合成与杀菌活性研究[J].农药学学报,2016,(1):28-36,9.基金项目
辽宁省自然科学基金(2015020766)；辽宁省教育厅优秀人才项目(LJQ2012059)；国家自然科学基金(31101466) （2015020766）
