Design, synthesis and fungicidal activity of novel 2-substituted aminocycloalkylsulfonamides

文献类型: 外文期刊

第一作者: Wang, Minlong

作者: Wang, Minlong;Qin, Peiwen;Qi, Zhiqiu;Ji, Mingshan;Li, Xinghai;Liu, Xingyu;Babu, P. Vijaya;Cui, Zi-Ning;Yan, Xiaojing

作者机构:

关键词: 2-Aminocycloalkylsulfonamides;Botrytis cinerea;Fungicidal activity;Structure-activity relationship

期刊名称:BIOORGANIC & MEDICINAL CHEMISTRY LETTERS ( 影响因子:2.823; 五年影响因子:2.677 )

ISSN:

年卷期:

页码:

收录情况: SCI

摘要: A series of novel 2-substituted aminocycloalkylsulfonamides were designed and synthesized by highly selective N-alkylation reaction, whose structures were characterized by H-1 NMR, C-13 NMR and HRMS. Among them, the configuration of compounds III12 and III20 were confirmed by X-ray single crystal diffraction. Bioassays demonstrated that the title compounds had considerable effects on different strains of Botrytis cinerea and Pyricularia grisea. Comparing with positive control procymidone (EC50 = 10.31 mg/L), compounds III28, III29, III30 and III31 showed excellent fungicidal activity against a strain of B. cinerea (CY-09), with EC50 values of 3.17, 3.04, 2.54 and 1.99 mg/L respectively. Their in vivo fungicidal activities were also better than the positive controls cyprodinil, procymidone, boscalid and carbendazim in pot experiments. Moreover, the fungicidal activity of III28 (EC50 = 4.62 mg/L) against P. grisea was also better than that of the positive control isoprothiolane (EC50 = 6.11 mg/L). Compound III28 would be great promise as a hit compound for further study based on the structure-activity relationship. (C) 2016 Elsevier Ltd. All rights reserved.

分类号: R9

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