期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 64, 期 -, 页码 329-344出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.03.049
关键词
Benzimidazole; Antibacterial; Antifungal; Fluconazole; Norfloxacin; Chloromycin
资金
- National Natural Science Foundation of China [21172181, 81250110089, 81250110554]
- Natural Science Foundation of Chongqing [CSTC2012jjB10026]
- Specialized Research Fund for the Doctoral Program of Higher Education of China [SRFDP 20110182110007]
A novel series of benzimidazole type of Fluconazole analogues were synthesized and characterized by H-1 NMR, C-13 NMR, IR, MS and HRMS spectra. All the new compounds were screened for their antimicrobial activities in vitro by two-fold serial dilution technique. The bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles gave comparable or even stronger antibacterial and antifungal efficiency in comparison with reference drugs Chloromycin, Norfloxacin and Fluconazole. The combination of 2,4-difluorobenzyl benzimidazole derivative 5m and its hydrochloride 7 respectively with antibacterial Chloromycin, Norfloxacin or antifungal Fluconazole showed better antimicrobial efficiency with less dosage and broader antimicrobial spectrum than the separated use of them alone. Notably, these combined systems were more sensitive to Fluconazole-insensitive Aspergillus flavus and methicillin-resistant MRSA. (C) 2013 Elsevier Masson SAS. All rights reserved.
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