Synthesis and antifungal activity of 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluorophenyl)-3-(N-butyl-N-substituted benzylamino)-2-propanol
10.3724/SP.J.1008.2009.01052
- Author:
Ning WEI
1
Author Information
1. Outpatient Department
- Publication Type:Journal Article
- Keywords:
Antifungal agents;
N-butyl;
Structure-activity relationship;
Substituted benzyl;
Synthesis
- From:
Academic Journal of Second Military Medical University
2010;30(9):1052-1057
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To study the antifungal activity of triazole alcohols by introducing N-butyl and substituted benzyl as side chain. Methods: Fourteen title compounds were synthesized and characterized by 1H NMR, IR, and LC-MS. The MICs of the compounds were determined by in vitro test using 8 clinical pathogenic fungi. Results: The title compounds exhibited potent antifungal activities against nearly all fungi tested (except for Aspergillus fumigatus), especially for the deep infection ones. Compounds 6a, 6d, and 6j showed a 16-fold activity (with a MIC80 value of 0.0156 μg/ml) as that of fluconazole against Microsporum gypseum. Compounds 6m and 6n showed a 128-fold activity (with a MIC80 value of 0.0039 μg/ml) as that of fluconazole against Candida albicans, and their activities were higher than those of other positive controls. Conclusion: The title compounds with N-butyl and substituted benzyl all have antifungal activities.
