论文部分内容阅读
为了寻找新型高效低毒的抗真菌药，根据氮唑类抗真菌药物的构效关系和作用机理，设计合成了２１ 个２ ，２双取代４（２ ，４二氟苯基）４（１ Ｈ１ ，２ ，４三唑１基） 甲基１ ，３ 二氧戊环类化合物，其结构经元素分析及氢核磁共振谱证实．初步的体外抗真菌活性试验表明：所有的目标化合物对６ 种常见的致病真菌都有不同程度的抗真菌活性，对浅部真菌的效果要比对深部真菌的效果好，其中化合物（Ⅰ７） ，（Ⅰ１２） ，（ Ⅰ１３） ，（ Ⅰ１５）的活性与克霉唑或酮康唑相当，化合物（ Ⅰ１２） 对白念珠菌、新生隐球菌有很强的抑制作用．
In order to find a new antifungal agent with high toxicity and low toxicity, 21 2, 2-substituted 4 (2, 4-difluorophenyl) benzenes were designed and synthesized according to the structure-activity relationship and mechanism of azole antifungal agents. 4 (1 H 1, 2, 4 triazole 1 base) methyl 1, 3 dioxolane compounds, the structure was confirmed by elemental analysis and hydrogen nuclear magnetic resonance spectroscopy. Preliminary in vitro antifungal activity tests showed that all of the target compounds had different degrees of antifungal activity against six common pathogenic fungi and had a better effect on shallow fungi than deep fungi. Compound (I7) , (Ⅰ12), (Ⅰ13) and (Ⅰ15) were comparable to clotrimazole or ketoconazole. Compound (Ⅰ12) had a good inhibitory effect on Candida albicans and Cryptococcus neoformans.