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目的:为了寻找比伯喹毒性低、疗效好的疟疾根治药物,合成了4个2-取代苯氧基(甲氧基)-4-甲基伯喹的类似物。方法:用关键中间体2-氯-4-甲氧基-8-乙酰氨基喹啉(Ⅵ)与相应酚的钾盐缩合得到2-取代苯氧基-4-甲基-6-甲氧基-8-乙酰氨基喹啉(Ⅶ),Ⅶ用稀盐酸水解,得到相应的氨基化合物(Ⅷ),Ⅷ与N-(4溴戊基)-邻苯二甲酰亚胺缩合后经水合肼水解,成盐后得目标化合物Ⅳa~d。结果:经鼠疟P.bergheiK173株的抑制性治疗作用评价,化合物Ⅳa~d的ED90分别为125.11,75.37,72.12及3.16mg/kg。结论:该类化合物对鼠疟的抑制性治疗作用效果低于伯喹。
OBJECTIVE: In order to find a cure for malaria with low toxicity and good efficacy of biequine, four analogues of 2-substituted phenoxy (methyloxy) -4-methylprednisolone were synthesized. Methods: The key intermediate 2-chloro-4-methoxy-8-acetamidoquinoline (VI) was condensed with the corresponding potassium salt of phenol to give 2-substituted phenoxy-4-methyl-6-methoxy (VII), VII with dilute hydrochloric acid hydrolysis, to give the corresponding amino compounds (VIII), VIII and N- (4 bromopentyl) - phthalimide condensation hydrazine hydrolysis , Into the salt after the target compound IVa ~ d. Results: Murine malaria P. The inhibitory therapeutic effect of bergheiK173 strain was evaluated with ED90 of compounds IVa-d of 125.11, 75.37, 72.12 and 3.16 mg / kg, respectively. Conclusion: The inhibitory effects of these compounds on murine malaria are less effective than primaquine.