亲脂性N-烷基二胺的制备及其抗利什曼原虫活性
Preparation and antileishmanial activity of lipophilic N-alkyl diamines.
作者信息
da Costa Cristiane F, Coimbra Elaine S, Braga Fernanda G, dos Reis Roberta C N, da Silva Adilson D, de Almeida Mauro V
机构信息
Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Cidade Universitária, Campos Martelos, Juiz de Fora, MG, Brazil.
出版信息
Biomed Pharmacother. 2009 Jan;63(1):40-2. doi: 10.1016/j.biopha.2007.12.013. Epub 2008 Jan 18.
We report in this work the preparation and the in vitro antileishmanial activity of a series of long chains N-monoalkylated diamines and two pyridinediamine derivatives. Several compounds, tested for their in vitro antiproliferative activity against Leishmania amazonensis and Leishmania chagasi, displayed a good inhibition of parasite growth, with IC(50) below 10 microM. Compounds 10 (N-dodecyl-1,2-ethanediamine), 15 (N-decyl-1,3-propanediamine) and 20 (N-dodecyl-1,4-butanediamine) were 7.3, 2.6 and 3.6 times, respectively, more active than the reference drug amphotericin B against L. chagasi promastigote forms.
我们在这项工作中报告了一系列长链N-单烷基化二胺和两种吡啶二胺衍生物的制备及其体外抗利什曼原虫活性。几种化合物针对亚马逊利什曼原虫和恰加斯利什曼原虫进行了体外抗增殖活性测试，显示出对寄生虫生长的良好抑制作用，半数抑制浓度（IC50）低于10微摩尔。化合物10（N-十二烷基-1,2-乙二胺）、15（N-癸基-1,3-丙二胺）和20（N-十二烷基-1,4-丁二胺）对恰加斯利什曼原虫前鞭毛体形式的活性分别比参考药物两性霉素B高7.3倍、2.6倍和3.6倍。
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