抗血吸虫药物硝唑酰化物及其类似物的合成  

SYNTHESIS OF ACYLATES OF NIRIDAZOLE AND ITS ANALOGS AS SCHISTOSOMICIDES

作　　者：马桢[1] 司保训[2] 刘意玲 黄兰孙 

机构地区：[1]中国预防医学科学院寄生虫病研究所,上海200025 [2]山东省医学科学院药物研究所

出　　处：《药学学报》1989年第6期476-480,共5页Acta Pharmaceutica Sinica

摘　　要：硝唑眯(Ⅰ)是六十年代发现的抗曼氏及埃及血吸虫药物。对日本血吸虫也有治疗作用,但毒副反应较大,应用受到限制。考虑到药物分子中氨基经酰化后毒性往往降低的一般规律,我们设计合成了一系列硝唑咪酰化物。In order to decrease the toxicity and enhance the curative effec tof niridazole against Schistosomiasis japonica, a series of acylates of niridazole has been prepared through acylation of niridazole with appropriate acid chlorides or anhydrides. The analogs of niridazole, 2-substituted acetamido-5-nitrothiazoles and 1- (5-nitro-2-thiazolyl) -4-acylpiperazinse were also prepared. The products has been tested against Schistosomiasis japonica in mice.Preliminary test results showed that the majority of aliphatic acylates of niridazole exhibited marked schistosomicidal effect against adult worms as well as larva (compounds 2, 4～8, 12, 13, 15, 18, 19),a few of aromatic and heterocyclic acylates (compounds 14, 22) and the analogs of niridazole (compounds 26, 39, 49) showed weak activity.

关 键 词：抗血吸虫病药 硝唑咪酰化物 硝唑咪 

分 类 号：R978.65[医药卫生—药品]