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本文报道了根据羟基哌喹、12,278RP及M1020的结构和生物活性的特点设计合成的一类高效抑制性抗疟化合物。经鼠疟初筛,化合物Ⅳ_(c,g,h)3 mg/kg连续灌服3天,原虫抑制率可达99.9~100%。鼠疟抑制性预防试验中,化合物Ⅳ_a和Ⅳ_(d2)有明显的长效作用,IVd_2一次灌服600 mg/kg可在45天内保护小鼠不被红内期伯氏原虫感染,它对恒河猴输血感染食蟹猴疟原虫的保护期为20~25天。
In this paper, a series of highly effective and inhibitory antimalarial compounds were designed and synthesized according to the structures and biological activities of hydroxyperpequine, 12,278RP and M1020. After malaria screening, the compound Ⅳ_ (c, g, h) 3 mg / kg for 3 consecutive days, the protozoa inhibitory rate of 99.9 to 100%. Compounds Ⅳ_a and Ⅳ_ (d2) showed significant long-term effects in the inhibition test of murine malaria. Once administered with 600 mg / kg IVd_2, the mice were protected from Bordetella pertussis infection within 45 days. Blood monkeys infected with rhesus monkeys malaria parasite protection period of 20 to 25 days.