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Synthesis of novel fluconazoliums and their evaluation for antibacterial and antifungal activities

European Journal of Medicinal Chemistry 46(9):4391 (2011) PMID 21794961

A series of novel fluconazoliums were synthesized and their bioactive evaluation as potential antibacterial and antifungal agents were described. Some target compounds displayed good and broad-spectrum antimicrobial activities with low MIC values ranging from 0.25 to 64 μg/mL against all the tested strains, including three Gram-positive bacteria ( Staphylococcus aureus, MRSA and Bacillus subtilis), three Gram-negative bacteria ( Escherichia coli, Pseudomonas aeruginosa and Bacillus proteus) as well as two fungi ( Candida albicans and Aspergillus fumigatus). Among all tested title compounds, the octyl, dichlorobenzyl, naphthyl and naphthalimino derivatives gave comparable or even better antibacterial and antifungal efficiency in comparison with the reference drugs Fluconazole, Chloromycin and Norfloxacin.

DOI: 10.1016/j.ejmech.2011.07.010