邓蓉仙, 余礼碧, 张洪北, 耿荣良, 叶克龙, 张德芳. 抗疟药的研究——α-(烷氨基甲基)-卤代-4-芴甲醇类化合物的合成J. 药学学报, 1981, 16(12): 920-924.
引用本文: 邓蓉仙, 余礼碧, 张洪北, 耿荣良, 叶克龙, 张德芳. 抗疟药的研究——α-(烷氨基甲基)-卤代-4-芴甲醇类化合物的合成J. 药学学报, 1981, 16(12): 920-924.
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Deng Rongxian, Yu Libi, Zhang Hongbei, Geng Rongliang, Ye Kelong , Zhang Defang, . STUDIES ON ANTIMALARIAL AGENTS——α-(ALKYLAMINOMETHYL)-HALOGENATED-4-FLUORENEMETHANOLSJ. Acta Pharmaceutica Sinica, 1981, 16(12): 920-924.
Citation: Deng Rongxian, Yu Libi, Zhang Hongbei, Geng Rongliang, Ye Kelong , Zhang Defang, . STUDIES ON ANTIMALARIAL AGENTS——α-(ALKYLAMINOMETHYL)-HALOGENATED-4-FLUORENEMETHANOLSJ. Acta Pharmaceutica Sinica, 1981, 16(12): 920-924.
shu

抗疟药的研究——α-(烷氨基甲基)-卤代-4-芴甲醇类化合物的合成

STUDIES ON ANTIMALARIAL AGENTS——α-(ALKYLAMINOMETHYL)-HALOGENATED-4-FLUORENEMETHANOLS

    摘要
  • 摘要: 本文报道α-(烷氨基甲基)-7-溴-4-芴甲醇Ⅰ和α-(烷氨基甲基)-2,7-二氯-4-芴甲醇Ⅱ的合成。动物筛选的初步结果表明,这两类化合物均有一定的抗鼠疟作用。Ⅱ类化合物的抗疟作用比Ⅰ类化合物的强,Ⅱ类中的大多数化合物用25mg/kg的剂量即能抑制感染伯氏鼠疟原虫株(Plasmodium berghei berghei NK 65)小白鼠的原虫血症,其中Ⅱg,Ⅱh和Ⅱi用5mg/kg的剂量也能达到完全抑制。

     

    Abstract: Eight a-(alkylaminomethyl)-7-bromo-4-fluorenemethanols Ⅰ and twelve α-(alkylaminomethyl)-2,7-dichloro-4-fluorenemethanols Ⅱ have been synthesized and evaluated for antimalarial activity. Preliminary results Showed that some of these compounds displayed marked antimalarial activity against blood-induced plasmodium berghei in mice at 25 mg/kg.Compounds Ⅱ exhibited greater activity than compounds Ⅰ.The most active compounds were Ⅱg Ⅱh and Ⅱi which suppressed parasitemia at 5 mg/kg. None of these compounds showed any acute toxicity at the dosages tested.

     

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