新型三唑类衍生物的合成及其抗真菌活性研究

Synthesis and antifungal activities of novel triazole derivatives

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H 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MIC_(80)值<0.125μg/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。

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 1 H 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 com-pounds exhibited potent antifungal activities .Compound 1c showed high activities against 7 funguses except Aspergillus fumigatus with the MIC80 values less than 0.125μg/ml, which was 16 times higher than that of Voriconazole .Conclusion The title compounds with naphthalene and alkyl substituent showed potent antifungal activities .