4.2 Article

SYNTHESIS AND ANTIFUNGAL ACTIVITY EVALUATION OF 1-(2-BENZYLOXY-2-PHENYLETHYL)-1,2,3-TRIAZOLE MICONAZOLE ANALOGS

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PHARMACEUTICAL CHEMISTRY JOURNAL
卷 55, 期 5, 页码 436-440

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SPRINGER
DOI: 10.1007/s11094-021-02440-x

关键词

1,2,3-triazole; Miconazole analogs; Click Chemistry; antifungal

资金

  1. CONACYT [A1-S-18230, CVU: 388438, CVU: 173992]

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A series of 1-(2-aryloxy-2-phenylethyl)-1,2,3-triazole derivatives, synthesized via copper catalyzed azide-alkyne cycloaddition, showed potential antimicrobial activity against Candida genus strains and filamentous fungi. One derivative exhibited remarkable selectivity comparable to that of Itraconazole against Rhizopus oryzae.
A series of 1-(2-aryloxy-2-phenylethyl)-1,2,3-triazole derivatives (Miconazole analogs) was obtained via copper catalyzed azide-alkyne cycloaddition as the key step. The synthesized compounds were evaluated for antimicrobial activity against Candida genus strains as well as filamentous fungi (Mucor hiemalis, Aspergillus fumigatus and Rhizopus oryzae). A 1-(2-aryloxy-2-phenylethyl)-1,2,3-triazole derivative exhibited remarkable selectivity comparable to that of Itraconazole against Rhizopus oryzae.

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