1-(1H-1,2,4-三唑-1-基)-2-(2,4-二氟苯基)-3-取代氨基-2-丙醇的合成及其抗真菌活性

SYNTHESIS AND ANTIFUNGAL ACTIVITIY OF 1 (1 H 1,2,4 TRIAZOL 1 YL) 2 (2,4 DIFLUOROPHENYL) 3 SUBSTITUTED AMINO 2 PROPANOLS

根据氮唑类抗真菌药物的构效关系，设计合成了８个１－（１Ｈ－１，２，４－三唑－１－基）－２－（２，４－二氟苯基）－３－取代氨基－２－丙醇类化合物。体外抗真菌活性试验表明，该类化合物对几种常见的浅部致病真菌有一定活性，对深部真菌的活性较弱，其中化合物１ａ、１ｂ对卡氏枝孢霉菌的活性比氟康唑强。

According to the structure activity relationship and antimycotic mech anism of azole compounds, eight 1 (1 H 1,2,4 triazol 1 yl) 2 (2,4 difluorophenyl) 3 substituted amino 2 propanols 1 a～h were designed and synthesized. The results of in vitro antifungal test showed that the title compounds exhibited mild activities a against the tested dermophytes, but low activities against systemic pathogenic fungi. The activites of 1 a and 1 b against Cladosporium carrioni were more potent than that of fluconazole.