Synthesis of 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluoro-phenyl)-3- N-cyclopropyl-N-substituted amino-2-propanols and test of its antifungal activity

Author: Qing-Jie ZHAO ¹
Author Information

1. Department of Organic Chemistry
Publication Type:Journal Article
Keywords: Antifungal activity in virtro; Cyclopropyl; Medicinal chemistry; Triazoles
From: Academic Journal of Second Military Medical University 2010;30(2):198-201
CountryChina
Language:Chinese
Abstract: Objective: To study the antifungal activity of triazole alcohols by introduction of cyclopropyl as side chain. Methods: Nine title compounds were synthesized and characterized by 1 HNMR, MS spectra and element analysis. Eight fungi were used for in vitro anti-fungal test. Results: All of the title compounds showed antifungal activities of different extents, especially to the deep infection ones,and they had a MIC value < 0.125 μg/ml against Candida albicans,showing an anti-fungal activity 4 times higher than that of fluconzole and similar to that of totraconazaole. Conclusion: 1-(1H-1,2,4-triazole-1-yl)-2-(2, 4-difluoro-phenyl)-3-[N-cyclopropyl-N-(3,4-dichlorobenzyl) amino]-2-propanols (6f) has a better activity ratio and is worth further studying.