抗疟药的研究——Ⅱ.α-烷氨基甲基-1,6-二氯-4-芴甲醇类化合物的合成
STUDIES ON ANTIMALARIALS Ⅱ.SYNTHESIS OF α-ALKYLAMINOMETHYL-1,6-DICHLORO-4-FLUORENEMETHANOLS
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摘要: 本文报道合成了14个α-烷氨基甲基-1,6-二氯-4-芴甲醇(Ⅱ)盐酸盐。初步动物筛选结果表明,大多数化合物在25~100 mg/kg的剂量对鼠疟有抑制性治疗作用,其中Ⅱr在剂量为2.5 mg/kg即能抑制原虫血症。Abstract: The preceding paper of this series described; the antimalarial activity of α-alkylaminomethyl-halogenated-4-fluorenemethanols. In order to search for further antimalarials with higher activity and lower toxicity, a series of another fourteen α-alkylaminomethyl-1,6-dichloro-4-fluorenemethanols (Ⅱ) wassynthesized for biological evaluation. Preliminary results showed that nine of the compounds were active at 25 mg/kg; among them Ⅱ suppressed parasitemia at 2.5 mg/kg.
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