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抗血吸虫病新药S72014,1-(5-硝基-2-噻唑)-3-二异丁氨基甲基-四氢咪唑酮-2及其同系物,系以硝唑咪为原料,与相应的第二胺及甲醛用曼氏反应合成。S72014和它的绝大多数同系物对小白鼠、兔及猴体内的日本血吸虫都有显著的杀灭作用。S72014对小白鼠的毒性比硝唑咪低达10倍,其化疗指数则高达硝唑咪的3.5倍。用小白鼠进行的S72014与硝唑咪对化学惊厥药物影响的实验表明,S72014在剂量大于硝唑咪引起惊厥的剂量10倍时,没有影响。本文还略论了S72014和它的同系物的构效关系。
Anti-schistosomiasis new drug S72014, 1- (5-nitro-2-thiazole) -3-diisobutylaminomethyl-tetrahydroimidazolone-2 and its homologues, Department of nitazoxanide as raw materials, and the corresponding The second amine and formaldehyde Mann’s reaction synthesis. S72014 and most of its homologues have significant killing effects on Schistosoma japonicum in mice, rabbits and monkeys. S72014 on mice toxicity than nifedipine as low as 10 times, its chemotherapy index is as high as 3.5 times nifedipine. Experiments with S72014 and nifedipine on the effects of chemoconvulsive drugs using mice showed that S72014 had no effect at doses larger than 10 times the dose of nifedipine induced convulsions. This article also briefly discusses the structure-activity relationship of S72014 and its homologues.