In order to investigate the synthesis of triazole antifungal agents, and biological activity testing, will difluorobenzene as the starting material, the use of Fu Reed-carat Crafts Reaction(hereinafter referred to as "Fu - Crafts Reaction")synthesis intermediate substance, and then after condensation, methylene transfer, and other open-loop synthesis prepared fluconazole. Select Candida albicans and Aspergillus Niger as a reference test antibacterial activity, the use of PDA culture method two fungi inoculation fluconazole synthesis and antibacterial activity recorded. Depending on the selected control drugs and antibacterial activity of fluconazole comparative experiments showed that the inhibition of control drug fluconazole and Candida albicans is very obvious, but no significant inhibition of Aspergillus Niger, while the inhibitory effect of fluconazole significantly higher than the control drugs. From this, three azole antifungals is a synthetic antibacterial drugs, the synthesis process can be completed in the laboratory, is simple, while the drug inhibition of fungal obviously has great clinical value.%为了探讨三氮唑类抗真菌药物的合成方法和生物活性检测,将间二氟苯作为原料,采用傅里德-克拉夫茨反应(下简称"傅-克反应")合成中间体物质,再经过缩合、亚甲基转移、开环等合成反应制得氟康唑.选择白色念珠菌和黑曲霉作为抑菌活性检验参照物,利用PDA培养法培养两种真菌,接种合成氟康唑,并记录抑菌活性.根据选择的对照药物和氟康唑抑菌活性对比实验显示,氟康唑和对照药物对白色念珠菌的抑制作用非常明显,但对黑曲霉的抑制作用不明显,同时氟康唑的抑菌作用明显高于对照药品.由此可知,三氮唑类抗真菌药物是一种合成抗菌药物,其合成过程可在实验室内完成,较为简便,同时这种药物对真菌的抑制作用比较明显,具有极大的临床应用价值.
展开▼
