2—（2，4—二氟苯基）—3—（N—甲基—N—取代磺酰胺基）—1—（1H—1，2，4—三唑—1—基）—2—丙醇的合成和抗真菌活性的研究

本文设计合成了10个新的具有3－取代磺酰胺基－2－芳基－1－三唑基结构特征的三氮唑类化合物作为真菌细菌色素P450 14α－去甲基化酶的抑制剂。体外抗真菌活性试验表明化合物1b,1c,和1g对白色念珠菌，近平滑念珠菌和裴氏着色菌具有较强的抑菌活性，但总体来说活性不如酮康唑。与标准对照品氟康唑相比，化合物1b,1c和1g对近平滑念珠菌的作用分别比氟康唑强32倍，16倍和4倍；对裴氏着色菌的抑制作用分别双氟康唑强4倍，8倍和8倍。

Synthesis and Antifungal Activities of 2-(2,4-Difluorophenyl)-3- (N-Methyl-N-Substituted Sulfonamido )-1-(1H-1,2,4-Triazol-1-yl)-2- Propanol

Ten new antifungal triazoles, 3-sulfonamido-2-aryl-1-triazoly-2-propanol derivatives were designed and synthesized as potential inhibitors of the fungal cytochrome P-450 14a-demethylase. Results of antifungal tests in vitro showed that compounds 1b, 1c and 1g had high activity, especially against Candida albicans, Candida parapsilosis and Fonsecaea pedrosor, but less active in comparison with ketoconazole. Compared with fluconazole, compound 1b was thirty-two times more active against Candida parapsilosis and four times more active against Fonsecaea pedrosor, compound 1c was sixteen times more active against Candida parapsilosis and eight times more active against Fonsecaea pedrosor, compound 1g was four times and eight times more active against Candida parapsilosis and Fonsecaea pedrosor respectively.