A facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity

Four novel miconazole analogues (8–11) were synthetized and evaluated for activity against four filamentous fungi (Mucor hiemalis, Aspergillus fumigatus, Trichosporon cutaneum, and Rhizopus oryzae) and eight species of Candida as yeast specimens. Compounds 9 and 10 showed very good activity when evaluated in yeast (MIC 0.112 and 0.163 μg/mL) compared to the reference compound, itraconazole (MIC 0.067 μg/mL). The best antifungal activity in filamentous strains was shown by compound 9. Hence compounds 9 and 10 represent new leads for further pharmacomodulation in this series. [Display omitted] •Miconazole analogues were synthetized through a facile synthetic strategy.•Evaluation against filamentous and yeast fungi.•Two of these compounds showed significant biological properties.•These results were consistent for both ATCC strains and clinical isolates.