Emami Saeed, Foroumadi Alireza, Falahati Mehraban, Lotfali Ensieh, Rajabalian Saeed, Ebrahimi Soltan-Ahmed, Farahyar Shirin, Shafiee Abbas
Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari 48175, Iran.
Bioorg Med Chem Lett. 2008 Jan 1;18(1):141-6. doi: 10.1016/j.bmcl.2007.10.111. Epub 2007 Nov 4.
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 microg/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.
2-羟基苯甲酰唑和2-羟基苯甲酰唑鎓化合物已被描述为一类新型的唑类抗真菌剂。大多数目标化合物对测试真菌（白色念珠菌、酿酒酵母、黑曲霉和石膏样小孢子菌）显示出显著的体外抗真菌活性，其低最小抑菌浓度（MIC）值在0.25 - 32微克/毫升范围内，与参考药物氟康唑相当。还使用MTT比色法在正常小鼠成纤维细胞（NIH/3T3）上评估了最具活性的化合物的细胞毒性。抗真菌活性和毒性测试结果表明，这些化合物在无细胞毒性的浓度下表现出抗真菌活性。
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