【摘要】 我所生化代谢的研究发现氟乙酸钠有显著的杀日本血吸虫的作用,作者等据此合成了125个氟乙酰胺类化合物。动物实验治疗结果证明,122个化合物有抗血吸虫作用,其中21个化合物的减虫率达90～100％,而毒性较之氟乙酸大幅度地降低,有些化合物剂量可高达5～10mg/鼠,但离进行临床试验还有一定的差距。更多还原

【Abstract】 Huang T Y and coworkers had observed the significant schistosomicidal effect of sodium fluoroacetate in the study of carbohydrate metabolism of S. japonicum. This fact 1ed us to synthesize the fluoroacetic acid derivatives of lower toxicity. One hundred and twenty-five fluoroacetamides were prepared and submitted for animal screening tests and experimental therapy. Most of the fluoroacetamides showed prominent, antischistosomal activity and much lower toxicity than that of fluoroacetic acid. However, they were still rather toxic for clinical trial.更多还原