【摘要】 <正> 近年来关于抗血吸虫药物的研究,在治疗上已取得了优异的成果,如吡喹酮的研究和应用,在预防药物研究方面,意义虽属重大,也偶见报道,但却进展缓慢。氯硝柳胺(5,2′-二氯-4′-硝基水杨酰苯胺)是目前常用的杀螺药,兼有显著的杀血吸虫尾蚴的作用,为寻找血吸虫的预防药及早期治疗药的研究提供了途径。有关氯硝柳胺结构改造的报道,主要为改变水杨酰苯胺的取代基团和取代位置。鉴此,我们以氯硝柳胺为中心,扩大其研究范围,即保留水杨酰胺的基本结构,将芳胺改为脂肪胺,合成了5-氯水杨酰胺类(Ⅰ)和水杨酰胺N-Mannich碱(Ⅱ)。鉴于氯硝柳胺各种胺盐的研究并应用在杀螺及驱绦更多还原

【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.更多还原