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

Yi-Yi YY Zhang, Jia-Li JL Mi, Cheng-He CH Zhou, and Xiang-Dong XD Zhou

Eur J Med Chem 46(9):4391-402 (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.

Copyright © 2011 Elsevier Ltd. All rights reserved.

DOI: 10.1016/j.ejmech.2011.07.010
Version: za2963e q8zaf q8zb4 q8zc2 q8zd5 q8zee q8zf1 q8zg5

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