治疗钩端螺旋体病新药——盐酸甲唑醇及其衍生物的合成
THE SYNTHESIS OF "METHIMIDOL" AND ITS DERIVATIVES——A NEW ANTILEPTOSPIROSIS DRUG.
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摘要: 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。Abstract: 1-(2′-Hydroxyethyl)-2-methylimidazole (Ⅲ)and its hydrochloride was found to be effective against L. icterohaemorrhagiae infection in golden hamster animal model. Ⅲ. HCl named as "Methimidel" has been effectively used in clinical therapy.Twenty-seven derivatives of Ⅲ were prepared in our laboratory. Most esters of Ⅲ and all organic salts were shown to have significant effect against L. icterohaemorrhagiae in vivo, but the latter were shown to be nonhydroscopic whereas other are.
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