期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 23, 期 7, 页码 1481-1491出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.02.011
关键词
Antifungal activity; Azole antifungals; Fluconazole; Triazoles; Lanosterol 14 alpha-demethylase
资金
- Research Council of Mazandaran University of Medical Sciences, Sari, Iran
In order to find new azole antifungals, we have recently designed a series of triazole alcohols in which one of the 1,2,4-triazol-1-yl group in fluconazole structure has been replaced with 4-amino-5-aryl-3-mercapto-1,2,4-triazole motif. In this paper, we focused on the structural refinement of the primary lead, by removing the amino group from the structure to achieve 5-aryl-3-mercapto-1,2,4-triazole derivatives 10a-i and 11a-i. The in vitro antifungal susceptibility testing of title compounds demonstrated that most compounds had potent inhibitory activity against Candida species. Among them, 5-(2,4-dichlorophenyl)-triazole analogs 10h and 11h with MIC values of <0.01 to 0.5 mu g/mL were 4-256 times more potent than fluconazole against Candida species. (C) 2015 Elsevier Ltd. All rights reserved.
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