| 新型三唑类衍生物的合成及其抗真菌活性研究 |
| 投稿时间：2014-04-16 修订日期：2014-04-29 点此下载全文 |
| 引用本文：吴茂诚,李翔,吴秋业.新型三唑类衍生物的合成及其抗真菌活性研究[J].药学实践杂志,2014,32(3):186~190 |
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| 基金项目:国家自然科学基金(20192188). |
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| 中文摘要:目的 研究具有萘苄结构的三唑醇类化合物的抗真菌活性。方法 设计合成了9个目标化合物;其结构通过1H NMR、MS确证,选择8种真菌为实验菌株,根据美国国家临床实验室标准委员会(NCCLS)推荐的标准化抗真菌敏感性实验方法,进行体外抑菌活性测试。结果 所有化合物对所选真菌均表现出了一定的抑菌活性,化合物1c对除烟曲霉菌以外的其他7种真菌的MIC80值<0.125 μg/ml,是伏立康唑活性的16倍。结论 引入萘环和烃基侧链的目标化合物都有抗真菌活性。 |
| 中文关键词:三唑类衍生物 化学合成 抗真菌活性 |
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| Synthesis and antifungal activities of novel triazole derivatives |
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| Abstract:Objective To synthesize a new series of triazole compounds with naphthalene benzyl as side chain and evaluate the antifungal activity.Methods Nine title compounds were synthesized and determined by the 1H NMR and MS spectra. According to the method recommended by the national committee for clinical laboratory standards(NCCLS), the RPMI-1640 test medium was used,the antifungal activities of all the compounds were evaluated against eight human pathogenic fungi in vitro.Results The title compounds exhibited potent antifungal activities. Compound 1c showed high activities against 7 funguses except Aspergillus fumigatus with the MIC80 values less than 0.125 μg/ml, which was 16 times higher than that of Voriconazole. Conclusion The title compounds with naphthalene and alkyl substituent showed potent antifungal activities. |
| keywords:triazole derivatives chemical synthesis antifungal activity |
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