Zhou Y J, Zhang W N, Lu J G, Li K, Zhu J
Department of Medicinal Chemistry, College of Pharmacy, Second Military Medical University, Shanghai 200433.
Yao Xue Xue Bao. 1997 Dec;32(12):902-7.
Twenty-one 1-[2-[[(substituted-phenyl) methyl] thio]-2-(2, 4-difluorophenyl) ethyl]-1H-1,2,4-triazoles were synthesized and 19 compounds are reported for the first time. Results of biological tests in vitro showed that the antifungal activities of all title compounds were better than or comparable to the activities of fluconazole. The antifungal activities of compounds 1-7 and 11-17 were better than or comparable to the activities of sulconazole. Compounds 1, 2 and 5 were 512 times more active than sulconazole against epidermophyton floccosum; compound 5 was 32 times more active against Candida albicans, compound 2 was 32 times more active against Sporotrichum schenckii; compounds 2 and 14 were shown to be 64 and 32 times more active against Cryptococcus neoformans; compounds 1 and 5 were 16 times more active against Aspergillus fumigatus.
合成了21个1-[2-[[(取代苯基)甲基]硫代]-2-(2,4-二氟苯基)乙基]-1H-1,2,4-三唑，其中19个化合物为首次报道。体外生物测试结果表明，所有目标化合物的抗真菌活性均优于氟康唑或与之相当。化合物1-7和11-17的抗真菌活性优于或与舒康唑相当。化合物1、2和5对絮状表皮癣菌的活性比舒康唑高512倍；化合物5对白色念珠菌的活性高32倍，化合物2对申克孢子丝菌的活性高32倍；化合物2和14对新型隐球菌的活性分别高64倍和32倍；化合物1和5对烟曲霉的活性高16倍。
