论文部分内容阅读
据报道(5-硝基噻唑-2)-咪唑酮(简称硝唑咪,Ⅰ)具有杀灭埃及、曼氏和日本血吸虫作用,其抗血吸虫作用机制,似乎在于抑制虫体组织中6-磷酸葡萄糖脱氢酶的活力。经动物试验,每天给药100 mg/kg,连续给药10天,可杀死鼠体内所有血吸虫。国外已用于治疗埃及和曼氏血吸虫病;国内曾试用于日本血吸虫病临床,虽有治疗效果,但尚存在严重的中枢神经系统副作用,如出现精神兴奋、激动、幻觉、完全定向障碍、局部肌肉颤动和癫痫发作等。一般认为5-硝基噻唑是硝唑咪不可缺少的部分,同时也是使药物产生副作用的部分。为了试图降低药物的副作用,增加疗效,我们合成了一系列的N-位取代产物,加大了药物的分子,从而使硝
It has been reported that (5-nitrothiazol-2) -imidazolidone (hereinafter referred to as nitrazepam, Ⅰ) has the action of killing Egypt, Mann and Schistosoma japonicum, and its anti-schistosomiasis mechanism seems to be inhibiting the 6-phosphate Glucose dehydrogenase activity. Animal experiments, daily administration of 100 mg / kg, continuous administration of 10 days, can kill all the mice in vivo schistosomes. Abroad has been used to treat schistosomiasis in Egypt and Manchuria; domestic trials of schistosomiasis japonica clinical, although the treatment effect, but there are still serious side effects of the central nervous system, such as the emergence of mental excitement, excitement, hallucinations, complete disorientation, Muscle fibrillation and seizures. 5-nitrothiazole is generally considered an integral part of nitazoxanide, but also make part of the drug side effects. In an attempt to reduce the side effects of drugs and increase the therapeutic effect, we synthesized a series of N-substituted products and increased the molecular weight of the drug so that nitrate