Synthesis of Isatin Derivatives and the Biological Activity Against the Magnaporthe grisea

Plant Diversity ›› 2007, Vol. 29 ›› Issue (06): 717-721.

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Synthesis of Isatin Derivatives and the Biological Activity Against the Magnaporthe grisea

CHEN Gang^{1 , 4} , WANG Ye² , HE Hong-Ping¹ , LI Shun-Lin1 ,
ZHOU Li-Gang³ , HAO Xiao-Jiang^{1 , 2}

1 State Key Laboratory of Phytochemistry and Plant Resources in West China , Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204 , China ;

2 Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002 , China ;
3 College of Agronomy and Biotechnology , China Agricultur1 al University , Beijing 100094 , China;
4 Graduate University of Chinese Academy of Sciences, Beijing 100049 , China

Received:2007-05-14 Online:2007-12-25 Published:2007-12-25
Contact: HAO Xiao-Jiang

靛红衍生物的合成及其对稻瘟菌的生物活性

陈刚^{1 , 4} , 汪冶² , 何红平¹ , 李顺林¹ , 周立刚³ , 郝小江^{1 , 2}

1 中国科学院昆明植物研究所植物化学与西部植物资源持续利用国家重点实验室, 云南昆明 650204;
2 贵州省中科院天然产物化学重点实验室, 贵州贵阳 550002;
3 中国农业大学, 农学与生物技术学院, 北京 100094; 4 中国科学院研究生院, 北京 100049

通讯作者: 郝小江

Abstract

Abstract:

A series of 3-imine􊄯methylene-indole-2-one compounds was synthesized from isatin , and their activity on inhibition of germination of Magnaporthe grisea spores was evaluated . It was found that the hydroxymethyl and aminomethyl of N, and the methylene on C3 might be the pharmacophore . The p-substitute , hydroxy , and electron withdraw group of the aryl
methylene lead to poor activity , while the o- electron donor group leads to potent activity .

Key words: Magnaporthe grisea

摘要： 以靛红为原料合成了系列3-亚胺基􊄯亚甲基-吲哚-2-酮化合物及其Mannich 碱衍生物, 研究了它们在抗稻瘟菌方面的活性, 发现了这两种类型的若干化合物有较好的抑制稻瘟菌孢子萌发的活性, 初步讨论了构效关系。认为1 位的羟甲基和胺甲基、3 位的亚甲基是药效团, 芳基亚甲基苯环上对位取代基、羟基取代基和吸电子取代基不利于活性的提高, 邻位的供电子取代基有利于活性的提高。

关键词: 稻瘟菌, 靛红, 药效团

CLC Number:

Q 946

CHEN Gang^, , WANG Ye , HE Hong-Ping , LI Shun-Lin ,
ZHOU Li-Gang , HAO Xiao-Jiang^,. Synthesis of Isatin Derivatives and the Biological Activity Against the Magnaporthe grisea[J]. Plant Diversity, 2007, 29(06): 717-721.

陈刚1 , 4 , 汪冶2 , 何红平1 , 李顺林1 , 周立刚3 , 郝小江1 , 2 . 靛红衍生物的合成及其对稻瘟菌的生物活性[J]. Plant Diversity, 2007, 29(06): 717-721.

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Synthesis of Isatin Derivatives and the Biological Activity Against the Magnaporthe grisea

靛红衍生物的合成及其对稻瘟菌的生物活性

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