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2-取代苯基-2-氧代-、2-羟基-和2-酰氧基乙基磺酰胺的设计、合成及杀菌活性

Design, Synthesis and Fungicidal Activity of 2-Substituted Phenyl-2-oxo-, 2-Hydroxy- and 2-Acyloxyethylsulfonamides.

作者信息

Wang Minlong, Rui Peng, Liu Caixiu, Du Ying, Qin Peiwen, Qi Zhiqiu, Ji Mingshan, Li Xinghai, Cui Zining

机构信息

Department of Pesticide Science, Plant Protection College, Shenyang Agricultural University, Shenyang 110866, China.

State Key Laboratory for Conservation and Utilization of Subtropical Agro-Bioresources, Integrative Microbiology Research Centre, Guangdong Province Key Laboratory of Microbial Signals and Disease Control, South China Agricultural University, Guangzhou 510642, China.

出版信息

Molecules. 2017 May 4;22(5):738. doi: 10.3390/molecules22050738.

Abstract

Sulfonyl-containing compounds, which exhibit a broad spectrum of biological activities, comprise a substantial proportion of and play a vital role, not only in medicines but also in agrochemicals. As a result increasing attention has been paid to the research and development of sulfonyl derivatives. A series of thirty-eight 2-substituted phenyl-2-oxo- , 2-hydroxy- and 2-acyloxyethylsulfonamides were obtained and their structures confirmed by IR, ¹H-NMR, and elemental analysis. The in vitro and in vivo bioactivities against two strains, and , which differ in their sensitivity to procymidone, were evaluated. The in vitro activity results showed that the EC values of compounds and were 0.10, 0.01 mg L against the sensitive strain and 3.32, 7.72 mg L against the resistant strain , respectively. For in vivo activity against , compound and showed better control effect than the commercial fungicides procymidone and pyrimethanil. The further in vitro bioassay showed that compounds , and had broad fungicidal spectra against different phytopathogenic fungi. Most of the title compounds showed high fungicidal activities, which could be used as lead compounds for further developing novel fungicidal compounds against .

摘要

含磺酰基的化合物具有广泛的生物活性,不仅在药物中,而且在农用化学品中都占很大比例并发挥着至关重要的作用。因此,磺酰基衍生物的研究和开发受到越来越多的关注。我们合成了一系列38种2-取代苯基-2-氧代-、2-羟基-和2-酰氧基乙基磺酰胺,并通过红外光谱、¹H-核磁共振和元素分析确定了它们的结构。评估了这些化合物对两种对腐霉利敏感性不同的菌株的体外和体内生物活性。体外活性结果表明,化合物 和 对敏感菌株 的EC值分别为0.10、0.01 mg/L,对耐药菌株 的EC值分别为3.32、7.72 mg/L。对于对 的体内活性,化合物 和 表现出比市售杀菌剂腐霉利和嘧霉胺更好的防治效果。进一步的体外生物测定表明,化合物 、 和 对不同的植物病原真菌具有广泛的杀菌谱。大多数目标化合物表现出高杀菌活性,可作为进一步开发新型抗 杀菌化合物的先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4a67/6154733/dc28a90b2f7a/molecules-22-00738-g001.jpg

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