2-(2,4-二氟苯基)-3-(N 甲基-N-取代基酰胺基)-1-(1H-1,2,4-三唑-1-基)-2-丙醇类化合物的合成及抗真菌活性的研究  

SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF 2 (2,4 DIFLUOROPHENYL) 3 ( N METHYL N SUBSTITUTED ACYLAMINO) 1 (1H 1,2,4 TRIAZOL 1 YL) 2 PROPANOL

作　　者：钟武[1] 张万年[1] 李科[1] 周有骏[1] 朱驹[1] 吕加国[1] 

机构地区：[1]第二军医大学药学院,上海200433

出　　处：《药学学报》1999年第10期744-750,共7页Acta Pharmaceutica Sinica

基　　金：军队九五重点课题

摘　　要：目的：寻找新的高效、低毒、广谱的抗真菌药物。方法：设计合成了２１ 个三唑类化合物作为真菌细胞色素Ｐ４５０ １４α去甲基化酶的抑制剂，并通过体外抗真菌实验测定其抗真菌活性。结果：２１ 个化合物均为新化合物。体外抗真菌试验表明所有目标化合物对试验真菌均有不同程度的抑制作用，特别是对白色念珠菌和近平滑念珠菌具有很好的活性。结论：所有化合物都不同程度地对真菌细胞色素Ｐ４５０ １４α去甲基化酶有抑制作用，化合物１５ 对８ 种不同真菌均显示了较高的活性。AIM: To search for high efficacy, low toxicity and broad spectrum antifungal drugs. METHODS: Twenty one new triazole compounds were designed and synthesized as potential inhibitors of the fungal cytochrome P450 14α demethylase, and their antifungal activities were determined by biological tests in vitro . RESULTS: Biological tests showed that all compounds have antifungal activity especially against Candida albicans and Candida parapsilosis . CONCLUSION: All target compounds could be regarded as potential inhibitors. Compound 15 exhibited high activity in all antifungal tests and was worthy of advanced study as a potential drug.

关 键 词：三唑类 细胞色素 P450抑制剂 抗真菌活性 

分 类 号：R978.5[医药卫生—药品]