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

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.

Graphical abstractA series of new fluconazoliums were synthesized and evaluated for their antibacterial and antifungal activities in vitro. Some of them displayed broad antimicrobial spectrum and comparable or even better efficacy in comparison with the reference drugs.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Synthesis and characterization of a series of novel various fluconazoliums. ► Antibacterial and antifungal evaluation indicating broad antimicrobial spectrum. ► Comparable or superior antibacterial potency to Chloromycin and Norfloxacin for some fluconazoliums. ► Discussion for preliminary possible structure-activity relationships.