Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 9, Pages 4388-4398Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.06.012
Keywords
Antibacterial; Antifungal; Triazole; Imidazole; Benzimidazole
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Funding
- Natural Science Foundation of Chongqing (CSCT) [2007885369, 2009885296]
- Talents Introduction Foundation of Southwest University [SWUB2006018, XSGX0602]
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A series of novel amine-derived bis-azole compounds were designed by the systematical structural modification of Fluconazole and synthesized by a convenient and efficient method, and the antimicrobial activities for all prepared compounds were evaluated in vitro against six representative bacterial strains and two fungal strains. Bioactive results indicated that some synthesized compounds exhibited moderate or even better activities in comparison with the reference drugs. Especially. bis-imidazole 5b and its salts gave significant antibacterial efficacy against all tested bacteria strains including MRSA, while bis-triazoles 4b-c and their corresponding salts exhibited better activities against Candida albicans, Bacillus proteus than standard drugs Fluconazole and Norfloxacin respectively. Unexpectedly, bis-bromides 3a-f presented excellent activities against all tested microbial strains. (C) 2010 Elsevier Masson SAS. All rights reserved.
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