抗真菌剂的研究。17. C-5取代基对新型3,5-二取代异恶唑烷体外活性的影响。
Studies on antifungal agents. 17. Effects of the C-5-substitution on the in vitro activity of novel 3,5-substituted isoxazolidines.
作者信息
Dormer P A, Mullen G B, Mitchell J T, Allen S D, St Georgiev V
机构信息
Department of Organic Chemistry, Pennwalt Corporation, Rochester, N.Y.
出版信息
Chemotherapy. 1988;34(5):411-4. doi: 10.1159/000238600.
A number of novel 5-(substituted thiomethyl)-3-phenyl-3-(1H-imidazol-1-ylmethyl)-2- methylisoxazolidine derivatives were prepared and evaluated in vitro for antifungal activity in solid agar cultures against Trichophyton rubrum, Aspergillus fumigatus and Candida albicans. The effect of the 5-(substituted thiomethyl) group on the degree and scope of activity was studied and compared to that of the corresponding 5-phenoxymethyl and 5-[(substituted phenyl)thio(or amino)methyl] derivatives.
制备了一系列新型的5-（取代硫代甲基）-3-苯基-3-（1H-咪唑-1-基甲基）-2-甲基异恶唑烷衍生物，并在固体琼脂培养物中对红色毛癣菌、烟曲霉和白色念珠菌进行了体外抗真菌活性评估。研究了5-（取代硫代甲基）基团对活性程度和范围的影响，并与相应的5-苯氧基甲基和5-[(取代苯基)硫代(或氨基)甲基]衍生物进行了比较。
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