张照瑞, 刘贻孙. 氯硝柳胺脂肪胺盐和水杨酰胺化合物的合成及其杀螺、抗血吸虫活性J. 药学学报, 1986, 21(12): 935-938.
引用本文: 张照瑞, 刘贻孙. 氯硝柳胺脂肪胺盐和水杨酰胺化合物的合成及其杀螺、抗血吸虫活性J. 药学学报, 1986, 21(12): 935-938.
ZHANG Zhao-Rui, LIU Yi-Sun. STUDIES ON THE SYNTHESIS OF SALICYLAMIDES AND ALKAMINE SALTS OF NICLOSAMIDE AND THEIR ACTIVITIES AGAINST SCHISTOSOMA JAPONICUM AND ONCOMELANIAJ. Acta Pharmaceutica Sinica, 1986, 21(12): 935-938.
Citation: ZHANG Zhao-Rui, LIU Yi-Sun. STUDIES ON THE SYNTHESIS OF SALICYLAMIDES AND ALKAMINE SALTS OF NICLOSAMIDE AND THEIR ACTIVITIES AGAINST SCHISTOSOMA JAPONICUM AND ONCOMELANIAJ. Acta Pharmaceutica Sinica, 1986, 21(12): 935-938.

氯硝柳胺脂肪胺盐和水杨酰胺化合物的合成及其杀螺、抗血吸虫活性

STUDIES ON THE SYNTHESIS OF SALICYLAMIDES AND ALKAMINE SALTS OF NICLOSAMIDE AND THEIR ACTIVITIES AGAINST SCHISTOSOMA JAPONICUM AND ONCOMELANIA

  • Abstract: Two series of salicylamides (Ⅰ and Ⅱ) and alkamine salts of niclosamide (Ⅲ) have been prepared. Methyl salicylate was reacted with hydroperoxide and hydrochloric acid, and then condensed with amines to afford 5-chlorosalicylamides (Ⅰ). Reaction of salicylamide or 5-chloro-salicylamide with formaldehyde and cyclic aliphatic amine through Mannich reaction provided compounds (Ⅱ). Aliphatic amine salts of niclosamide (Ⅲ) were obtained by adding amines to niclosamide.Compounds of the Ⅲ series were found to possess pronounced activity against Oncomelania and cercaria of Schistosoma japonicum in mice. Among them compound Ⅲa exhibited a rather good cidal effect against 20-day-old immature Schistosomes by oral administration. But compounds of the Ⅰ and Ⅱ series showed no activity.

     

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