氮杂稠合若丹菁在体外及伯氏疟原虫小鼠模型中的合成与抗疟疗效
Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P. berghei mouse model.
作者信息
Takasu Kiyosei, Pudhom Khanitha, Kaiser Marcel, Brun Reto, Ihara Masataka
机构信息
Department of Organic Chemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Aobayama, Sendai 980-8578, Japan.
出版信息
J Med Chem. 2006 Jul 27;49(15):4795-8. doi: 10.1021/jm0606241.
Several aza-fused rhodacyanines were synthesized and assessed for their in vitro and in vivo antimalarial activities against Plasmodium falciparum K1 and P. berghei. All synthetic compounds showed strong selective antimalarial in vitro activity. Class II azarhodacyanines, 3, consisting of four heterocyclic units, were found to display good parasitemia suppression and low acute toxicity in vivo. Among them, 3c appeared to be the most effective at a dose of 20-25 mg kg(-1) day(-1) (ip).
合成了几种氮杂稠合的若丹明花青，并评估了它们对恶性疟原虫K1和伯氏疟原虫的体外和体内抗疟活性。所有合成化合物在体外均表现出较强的选择性抗疟活性。由四个杂环单元组成的II类氮杂若丹明花青3在体内显示出良好的抑制疟原虫血症作用和低急性毒性。其中，3c在剂量为20 - 25 mg kg(-1) 天(-1)（腹腔注射）时似乎最有效。
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