| 3,4-二氯异噻唑-5-甲酰胺衍生物的合成及生物活性 |
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| 引用本文： | 陈晓燕,戴良英,李岳东,毛武涛,房震,李娟娟,王盾,Tatiana KALININA,范志金. 3,4-二氯异噻唑-5-甲酰胺衍生物的合成及生物活性[J]. 农药学学报, 2013, 15(2): 140-144 |
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| 作者姓名： | 陈晓燕 戴良英 李岳东 毛武涛 房震 李娟娟 王盾 Tatiana KALININA 范志金 |
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| 作者单位： | 1.湖南农业大学 生物安全科学技术学院,长沙 410128 |
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| 基金项目： | 天津市自然科学基金重点项目(10JCZDJC17500);国家重点基础研究发展计划("973"计划)项目(2010CB126105);天津市农业科技成果转化与推广项目(201002250);天津市科技支撑计划重点项目(11ZCGYNC00100);国家科技支撑计划课题(2011BAE06B02)资助. |
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| 摘 要： | 异噻唑类杂环化合物具有广泛的生物活性。为了扩大先导结构的发现范围,以3,4-二氯异噻唑-5-甲酸为原料合成了10个未见文献报道的3,4-二氯异噻唑-5-甲酰胺衍生物;其结构经核磁共振氢谱、红外光谱和元素分析确证。初步生物测试结果表明,化合物Ⅲe对9种病原真菌表现出了广谱的抑菌活性,在50 μg/mL下其抑制率均超过50%;在100 μg/mL下,大部分化合物展现了较好的抗烟草花叶病毒(tobacco mosaic virus,TMV)或诱导烟草抗TMV活性,其中化合物Ⅲa和Ⅲi的诱导活性分别为41.88%和42.92%。
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| 关 键 词： | 异噻唑 合成 抑菌活性 植物激活剂 烟草花叶病毒 |
| 收稿时间： | 2013-01-04 |
| 修稿时间： | 2013-02-20 |
Synthesis and biological activity of 3,4-dichloroisothiazole-5-carboxylic amides |
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| CHEN Xiaoyan,DAI Liangying,LI Yuedong,MAO Wutao,FANG Zhen,LI Juanjuan,WANG Dun,Tatiana KALININA and FAN Zhijin. Synthesis and biological activity of 3,4-dichloroisothiazole-5-carboxylic amides[J]. Chinese Journal of Pesticide Science, 2013, 15(2): 140-144 |
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| Authors: | CHEN Xiaoyan DAI Liangying LI Yuedong MAO Wutao FANG Zhen LI Juanjuan WANG Dun Tatiana KALININA FAN Zhijin |
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| Affiliation: | 1.College of Biosafety Science and Technology, Hunan Agricultural University, Changsha 410128, China2.Jiangxi Tianren Ecological Co.Ltd., Jian 343100, Jiangxi Province, China3.State Key Laboratory of Elemento Organic Chemistry, Nankai University, Tianjin 300071, China4.The Ural Federal University Named After the First President of Russia B.N.Yeltsin, 620002, Ekaterinburg, Russia |
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| Abstract: | Isothiazole based heterocyclic compounds had various biological activities.In order to enlarge the library of novel elicitor lead with broad spectrum of highly systemic acquired resistance,a series of 3,4-dichloroisothiazole-5-carboxylic amides were synthesized by the reaction of carboxylic acid chlorination and condensation with 3,4-dichloroisothiazole-5-carboxylic acid as starting materials.All the ten novel compounds synthesized were confirmed by 1H NMR,IR and elemental analysis.Biological screening indicated that,compound Ⅲe presented broad-spectrum of fungicidal activity at 50 μg/mL against nine fungi with inhibition above 50%.Most compounds had good anti-tobacco mosaic virus(TMV) activity or systemic acquired resistance for tobacco against TMV at 100 μg/mL,among them,compound Ⅲa and Ⅲi exhibited 41.88% and 42.92% of good systemic acquired resistance for tobacco against TMV respectively. |
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| Keywords: | isothiazole synthesis bioactivity plant elicitor tobacco mosaic virus |
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