Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P-berghei mouse model
Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P-berghei mouse model
复制标题
DOI：
10.1021/jm0606241
复制
发表时间：
2006-07-27
影响因子：
7.3
通讯作者：
Ihara, Masataka
中科院分区：
文献类型：
--
作者：
Takasu, Kiyosei;Pudhom, Khanitha;Ihara, Masataka
合成了几种氮杂稠合的罗丹花青，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。所有合成化合物均表现出较强的选择性体外抗疟活性。第二类azarhodacyanines，3，由四个杂环单元组成，被发现在体内显示良好的寄生虫血症抑制和低急性毒性。其中，3c在20-25 mg kg-1 day-1（ip）剂量下似乎最有效。
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).