1-[2-(取代苯基甲硫基)-2-(2,4-二氟苯基)乙基]-1H-1,2,4-三唑类化合物的合成及抗真菌活性

设计合成了21个1-[2-(取代苯基甲硫基)-2-(2,4-二氟苯基)乙基]-1H-1,2,4-三唑类化合物,其中19个为首次报道。体外抑菌试验表明:所有目标化合物对8种试验真菌均有不同程度的抗菌活性,其中化合物1,2,5对絮状表皮癣菌的活性为硫康唑的512倍以上;化合物5对白色念株菌的活性为硫康唑的32倍;化合物2对申克孢子丝菌的活性为硫康唑的32倍;化合物2,14对新型隐球菌的活性分别为硫康唑的64倍,32倍;化合物1,5对熏烟色曲菌的活性分别为硫康唑的16倍以上。

SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF 1-{2-[(SUBSTITUTED-PHENYL) METHYL]THIO}-2-(2,4-DIFLUOROPHENYL)ETHYL-1H-1,2,4-TRIAZOLES

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.