2-Hydroxyphenacyl azoles and related azolium derivatives as antifungal agents

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• 作者：Saeed Emami ; Alireza Foroumadi ; Mehraban Falahati ; Ensieh Lotfali ; Saeed Rajabalian ; Soltan-Ahmed Ebrahimi ; Shirin Farahyar ; Abbas Shafiee
• 关键词：Azole ; Imidazole ; 1 ; 2 ; 4-Triazole ; 2-Hydroxyacetophenone ; Antifungal activity ; Cytotoxicity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：1 January 2008
• 年：2008
• 卷：18
• 期：1
• 页码：141-146
• 全文大小：156 K

文摘

2-Hydroxyphenacyl azole and 2-hydroxyphenacyl azolium compounds have been described as a new class of azole antifungals. Most target compounds showed significant in vitro antifungal activities against tested fungi (Candida albicans, Saccharomyces cerevisiae, Aspergillus niger, and Microsporum gypseum) with low MICs values included in the range of 0.25–32 μg/mL comparable to reference drug fluconazole. The most active compounds were also assessed for their cytotoxicity using MTT colorimetric assay on normal mouse fibroblast (NIH/3T3) cells. The results of antifungal activity and toxicity tests indicated that these compounds display antifungal activity at non-cytotoxic concentrations.