β-咔啉酰肼及酰胺衍生物的抑菌活性研究

摘要：我国每年因植物病害造成的农业生产减产高达15％，化学防治是目前最主要的控制病害方法。然而，随着杀菌剂长期、大量、不合理的使用，产生了农药残留、环境污染、病原物抗药性等问题。因此，开发新型农药变得尤为重要。咔啉类生物碱在自然界中种类多，分布广，具有抗癌、抑菌、杀虫等生物活性。本研究以L-色氨酸为原料合成了10个β-咔啉酰肼及酰胺衍生物，并测定了10个化合物对植物病原真菌和细菌的抑制活性。结果显示，化合物都对小麦全蚀病原菌表现出抑制活性，其中化合物4dq的EC50值为0.11ug/mL，远远低于阳性对照硅噻菌胺。化合物4dd和化合物4aa分别对马铃薯环腐病菌和丁香假单胞菌有抑制活性，MIC值分别为2ug/mL和8ug/mL，具有成为新型农用杀菌剂先导化合物的潜力。

关键词：β-咔啉酰肼；β-咔啉酰胺；抑菌活性；

Study on the antibacterial activity of β-carbarinamide and hydrazide derivatives

Abstract：Chemical control is the most important method to control plant diseases in China, which can reduce agricultural production by 15% every year. However, with the long-term, massive and unreasonable use of fungicides, there are problems such as pesticide residues, environmental pollution and resistance of pathogens. Therefore, it is very important to develop new pesticides. Carboline alkaloids are widely distributed in nature and have many kinds of biological activities, such as anticancer, bacteriostatic and insecticidal. In this study, 10 β-carbazide and amide derivatives were synthesized from L-tryptophan, and their inhibitory activities against plant pathogens and bacteria were determined. The results showed that all the compounds showed inhibitory activity against wheat take-all pathogen, and the EC50 value of compound 4dq was 0.11ug/mL, which was far lower than that of the positive control. Compound 4dd and compound 4aa had inhibitory activities against potato scab and pseudomonas clove, respectively, and MIC values were 2ug/mL and 8ug/mL, respectively, showing potential as lead compounds for new agricultural fungicides.

Key words: β-carbazide; β-carbazinamide; Bacteriostatic activity

摘要： 3

关键词： 3

Abstract： 3

Key words: 3

引言： 3

1 材料与方法 4

1.1 实验材料 4

1.2 化合物的合成 5

1.3 生物活性测定材料和菌种制备 5

1.3.1细菌菌种的活化 5

1.3.2真菌菌种的活化 5

1.4 β-咔啉酰胺及酰肼类衍生物的抗细菌活性测定 6

1.4.1抑菌圈的测定 6

1.4.2 最小抑菌浓度（MIC）的测定 6

1.5 β-咔啉酰胺及酰肼类衍生物的抗细菌活性温室实验 6

1.5.1 大豆叶片接种 6

1.5.2 药剂的喷施 6

1.6 β-咔啉酰胺及酰肼类衍生物的抗真菌活性测定 6

1.6.1抗真菌活性的初步测定 6

1.6.2待测化合物EC50的测定 6

1.7 β-咔啉酰胺及酰肼类衍生物的抗真菌活性温室实验 β-咔啉酰肼及酰胺衍生物的抑菌活性研究:http://www.chuibin.com/shengwu/lunwen_206226.html