三类罗丹明花青染料的合成及其体外和体内抗疟活性评估。
Synthesis of three classes of rhodacyanine dyes and evaluation of their in vitro and in vivo antimalarial activity.
作者信息
Pudhom Khanitha, Kasai Kazuki, Terauchi Hiroki, Inoue Hiroshi, Kaiser Marcel, Brun Reto, Ihara Masataka, Takasu Kiyosei
机构信息
Department of Organic Chemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Aobayama, Sendai 980-8578, Japan.
出版信息
Bioorg Med Chem. 2006 Dec 15;14(24):8550-63. doi: 10.1016/j.bmc.2006.08.035. Epub 2006 Sep 12.
Selected members of three classes of rhodacyanine dyes, [0,0]-, [1,0]-, and [0,0,0]-rhodacyanines, were synthesized and their in vitro antimalarial activities against Plasmodium falciparum K1 (chloroquine-resistant strain) as well as their in vivo activities against P. berghei in mice were determined. The novel [0,0,0]-rhodacynines, 3e and 3h, possessing a benzothiazole moiety, were shown to have highly promising antimalarial activities in vivo. Moreover, the [0,0,0]-rhodacyanines were found to be orally bioavailable.
合成了三类若丹花青素染料中的选定成员，即[0,0]-、[1,0]-和[0,0,0]-若丹花青素，并测定了它们对恶性疟原虫K1（氯喹抗性株）的体外抗疟活性以及对小鼠伯氏疟原虫的体内活性。具有苯并噻唑部分的新型[0,0,0]-若丹花青素3e和3h在体内显示出极有前景的抗疟活性。此外，发现[0,0,0]-若丹花青素具有口服生物利用度。
Zotero 插件