具有抗利什曼原虫活性的新型双苯并咪唑类化合物。
Novel bisbenzimidazoles with antileishmanial effectiveness.
作者信息
Mayence Annie, Pietka Aurélie, Collins Margaret S, Cushion Melanie T, Tekwani Babu L, Huang Tien L, Vanden Eynde Jean Jacques
机构信息
Xavier University of Louisiana, College of Pharmacy, Division of Basic Pharmaceutical Sciences, 1 Drexel Drive, New Orleans, LA 70125, USA.
出版信息
Bioorg Med Chem Lett. 2008 Apr 15;18(8):2658-61. doi: 10.1016/j.bmcl.2008.03.020. Epub 2008 Mar 10.
A small library of 2,2'-[(alpha,omega-alkanediylbis(oxyphenylene)]bis-1H-benzimidazoles has been prepared and screened in vitro against Pneumocystis carinii, Trypanosoma brucei rhodesiense, and Leishmania donovani. Among the six tested compounds two derivatives emerged as promising hits characterized by IC(50) values lower than that determined for pentamidine against L. donovani.
已制备了一个由2,2'-[(α,ω-亚烷基双(氧亚苯基)]双-1H-苯并咪唑组成的小型文库，并在体外针对卡氏肺孢子虫、布氏罗得西亚锥虫和杜氏利什曼原虫进行了筛选。在六种测试化合物中，有两种衍生物表现出有前景的活性，其半数抑制浓度（IC50）值低于针对杜氏利什曼原虫测定的喷他脒的IC50值。
Zotero 插件