| 杨丹,王平,吴汉福,李济澜.化学通报,2017,80(6):544-551. |
| 新型乙酰腙类化合物的合成与抗菌活性研究 |
| Synthesis and Antimicrobial Activity of novel Quinazolin-2,4-dione Acetyl Hydrazones |
| 投稿时间：2016-09-21 修订日期：2016-12-07 |
| DOI： |
| 中文关键词: 喹唑啉二酮 乙酰腙 合成 抗菌活性 |
| 英文关键词:Quinazolin-2,4-dione, Acetohydrazone, Synthesis, Antibacterial activity |
| 基金项目:贵州省科学技术厅联合基金 |
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| 中文摘要: |
| 以邻氨基苯甲酸甲酯为原料,经过甲基化、取代、关环、肼解反应制得含有喹唑啉二酮的中间体乙酰肼,进一步与多种取代醛和酮反应制得目标化合物9a-9t,所有化合物结构均经1H NMR、13C NMR、MS确证,并进行了体外抗菌活性测试,初步测试结果表明所有化合物均对测试菌株有一定的抗菌活性,且部分化合物对部分测试菌株的抑制活性接近甚至优于现有药物硫酸链霉素和多抗霉素B。 |
| 英文摘要: |
| Methyl 2-aminobenzoate was reacted with iodine methane to get methyl N-methylanthranilate. The key intermediate 2-(6-chloro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetohydrazide was synthesized from methyl N-methylan- thranilate via substitution, hydrolysis, cyclization and hydrazinolysis reactions. Then the key intermediate was reacted with various substituted aromatic aldehydes or ketones to afford a series of quinazolin-2,4-dione acetyl hydrazone compounds 9a-9t. The structures of all target compounds were characterized by means of 1H NMR、13C NMR、MS. The antimicrobial activities of these compounds were originally investigated. The preliminary bioassay indicated that these compounds had certain antibacterial activities against the tested strains. At the same time, some parts of as-synthesized compounds showed better antibacterial activities for tested strains than the existent drugs such as streptomycin sulfate and polyoxin B. |
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