Synthesis and antifungal activities of novel triazole derivatives

WU Maocheng; LI Xiang; WU Qiuye

doi:10.3969/j.issn.1006-0111.2014.03.006

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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.

Synthesis and antifungal activities of novel triazole derivatives

Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

Received Date: 2014-04-16

Rev Recd Date: 2014-04-29

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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.

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Reference (7)

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[7]	National Committee for Clinical Laboratory Standards.Reference method for broth dilution antifungal susceptibility testing of yeasts approved standard[S]. Document M27-A2, Wayne, PA, 2002.

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Synthesis and antifungal activities of novel triazole derivatives

doi: 10.3969/j.issn.1006-0111.2014.03.006

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通讯作者: 陈斌, [email protected]

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