通过亚胺狄尔斯-阿尔德反应制备的多官能化2-（杂）芳基喹啉的体外抗真菌活性
In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions.
作者信息
Meléndez Gómez Carlos M, Kouznetsov Vladimir V, Sortino Maximiliano A, Alvarez Sandra L, Zacchino Susana A
机构信息
Laboratorio de Química Orgánica y Biomolecular, Escuela de Química, Universidad Industrial de Santander, A.A. 678, Bucaramanga, Colombia.
出版信息
Bioorg Med Chem. 2008 Sep 1;16(17):7908-20. doi: 10.1016/j.bmc.2008.07.079. Epub 2008 Jul 29.
Diverse polyfunctionalized quinolines, easily prepared using Lewis acid-catalyzed imino Diels-Alder reactions between corresponding aldimines, were tested for antifungal properties against standardized as well as clinical isolates of clinically important fungi. Among them, 4-pyridyl derivatives displayed the best activities mainly against dermatophytes. The activity appears not to be related neither to the lipophilicity nor to the basicity of compounds.
通过相应醛亚胺之间的路易斯酸催化亚氨基狄尔斯-阿尔德反应易于制备的多种多官能化喹啉，针对临床上重要真菌的标准化菌株以及临床分离株进行了抗真菌特性测试。其中，4-吡啶基衍生物主要对皮肤真菌表现出最佳活性。该活性似乎与化合物的亲脂性和碱性均无关。
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