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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.