| 含2-甲基-5-硝基咪唑的吡酮酸类衍生物的合成及其抗菌活性含2-甲基-5-硝基咪唑的吡酮酸类衍生物的合成及其抗菌活性 |
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| 引用本文： | 叶发青,陈莉,黄金敏. 含2-甲基-5-硝基咪唑的吡酮酸类衍生物的合成及其抗菌活性含2-甲基-5-硝基咪唑的吡酮酸类衍生物的合成及其抗菌活性[J]. 药学学报, 2003, 38(4): 260-263 |
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| 作者姓名： | 叶发青 陈莉 黄金敏 |
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| 作者单位： | 1. 温州医学院,化学教研室,浙江,温州,325027
2. 咸宁医学院临床药学系,湖北,咸宁,437100 |
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| 基金项目： | 湖北省教育厅自然科学类重点课题资助项目(98B0 33) |
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| 摘 要： | 目的 研究含N-乙基-2-甲基-5-硝基咪唑的诺氟沙星、环丙沙星和依诺沙星衍生物的合成及其抗菌活性。方法 用含2-甲基-5-硝基咪唑的诺氟沙星、环丙沙星和依诺沙星等为原料,通过亲核取代、酯化合成目的物;测定目的物的抗菌活性。结果 设计、合成了9个新化合物(IIa～c,IIIa～f),其结构经MS,1HNMR和元素分析确证。化合物IIa～c的体内抗菌活性较明显。结论 化合物IIa～c显示了一定的体内抗菌活性,值得进一步研究。
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| 关 键 词： | 吡酮酸 前药 咪唑 抗菌活性 |
| 收稿时间： | 2002-04-21 |
Synthesis and antibacterial activity of pyridonecarboxylic acid derivatives containing 2-methyl-5-nitroimidazol |
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| YE Fa-qing,CHEN Li,HUANG Jin-min. Synthesis and antibacterial activity of pyridonecarboxylic acid derivatives containing 2-methyl-5-nitroimidazol[J]. Acta pharmaceutica Sinica, 2003, 38(4): 260-263 |
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| Authors: | YE Fa-qing CHEN Li HUANG Jin-min |
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| Affiliation: | Department of Chemistry, Wenzhou Medical College, Wenzhou 325027, China. YZYFQ-mail@sina.com |
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| Abstract: | AIM: To study the synthesis and antibacterial activity of pyridonecarboxylic acid derivatives containing 2-methyl-5-nitroimidazol. METHODS: Pyridonecarboxylic acid derivatives containing 2-methyl-5-nitroimidazol were synthesized primarily from 2-methyl-5-nitroimidazol, norfloxacin, ciprofloxacin, enoxacin via nucleophilic substitution and esterification. The antibacterial activity of the nine target compounds were tested. RESULTS: Nine new compounds were synthesized (IIa-c and IIIa-f). The structure of the title compounds were identified by 1HNMR, MS as well as elementary analysis. CONCLUSION: Compounds IIa, IIb and IIc showed antibacterial activity, and were worth further studying. |
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| Keywords: | pyridonecarboxylic acid prodrug imidaxole antibacterial activity |
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