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首页> 外文期刊>Medicinal chemistry >Discovery and Evaluation of Efficient Selenazoles with High Antifungal Activity Against Candida spp.
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Discovery and Evaluation of Efficient Selenazoles with High Antifungal Activity Against Candida spp.

机译：发现和评估对假丝酵母具有高抗真菌活性的硒氮唑。

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摘要

Synthesis, characterization and investigation of antifungal and antibacterial activities of fourteen 2,4-disubstituted 1,3-selenazoles is presented. Their structures were determined using H-1 and C-13 NMR, FAB MS and HRMS analyses. Among the derivatives, compounds 5, 6, 8, 9, 12, 13 and 15 had very strong activity against reference strains of C. albicans ATCC 10231 and C. parapsilosis ATCC 22019 with MIC = 0.24-7.81 mu g/ml. The compounds 5, 6, 8, 13 and 15 showed also very strong activity against clinical isolates belonging to non-albicans Candida spp. strains, i.e. C. krusei, C. inconspicua, C. famata, C. lusitaniae, C. sake, C. parapsilosis, C. dubliniensis with MIC = 0.24-7.81 mu g/ml. The activity of several of these was similar to the activity of most commonly used antifungal agents fluconazole. The compounds 9 and 16 indicate also very strong antibacterial activity against S. epidermidis and M. luteus with MIC = 1.95-3.91 mu g/ml. Additionally, the compound 11 is strong active against M. luteus with MIC = 3.91 mu g/ml.
机译：介绍了十四种2,4-二取代的1,3-硒仑唑的合成，表征和抗菌活性。使用H-1和C-13 NMR，FAB MS和HRMS分析确定其结构。在衍生物中，化合物5、6、8、9、12、13和15对白色念珠菌ATCC 10231和副念珠菌ATCC 22019的参考菌株具有非常强的活性，MIC = 0.24-7.81μg / ml。化合物5、6、8、13和15对非白色念珠菌属的临床分离株也显示出非常强的活性。菌株，即MIC = 0.24-7.81μg / ml的克鲁斯克鲁维酵母，无形梭菌，法氏梭菌，卢梭菌，清酒梭菌，近缘梭菌，杜氏梭菌。其中一些的活性类似于最常用的抗真菌剂氟康唑的活性。化合物9和16还显示出对表皮葡萄球菌和黄褐藻的非常强的抗菌活性，MIC ＝1.95-3.91μg/ ml。另外，化合物11对黄曲霉具有强活性，MIC ＝3.91μg/ ml。

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