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1-(2′-羟乙基)-2-甲基咪唑(Ⅲ)及其盐酸盐(Ⅲ·HCl)对金黄地鼠黄疽出血型钩端螺旋体病具有显著的治疗效果。 Ⅲ·HCl现定名为盐酸甲唑醇,临床治疗钩端螺旋体病患者281例,治愈率为94.31%。 合成1-(2′-羟乙基)-2-甲基咪唑(Ⅲ)的衍生物27个。Ⅲ的有机酸盐(11~15)和酯(16~25)对金黄地鼠黄疸出血型钩端螺旋体病大都有效,且有机酸盐无引湿性。
1- (2’-hydroxyethyl) -2-methylimidazole (Ⅲ) and its hydrochloride (Ⅲ · HCl) have significant therapeutic effect on golden hamster’s hemorrhagic leptospirosis. Ⅲ · HCl is now named metronidazole hydrochloride, clinical treatment of 281 cases of leptospirosis, the cure rate was 94.31%. Twenty-seven derivatives of 1- (2’-hydroxyethyl) -2-methylimidazole (Ⅲ) were synthesized. The organic acid salts (11-15) and esters (16-25) of III are mostly effective against hamster hemorrhagic leptospirosis, and organic acids do not induce hygroscopicity.