Parallel synthesis and antileishmanial activity of ether-linked phospholipids

被引:15
|
作者
Coghi, Paolo [1 ]
Vaiana, Nadia [1 ]
Pezzano, Maria G. [1 ]
Rizzi, Luca [1 ]
Kaiser, Marcel [2 ]
Brun, Reto [2 ]
Romeo, Sergio [1 ]
机构
[1] Univ Milan, Ist Chim Farmaceut & Tossicol Pietro Pratesi, I-20133 Milan, Italy
[2] Swiss Trop Inst, Dept Med Parasitol & Infect Biol, Socinstr 57, CH-4002 Basel, Switzerland
关键词
Leishmania donovani; ether-linked phospholipids; edelfosine; parallel synthesis; antiprotozoal activity;
D O I
10.1016/j.bmcl.2008.07.022
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and antileishmanial activity of 18 edelfosine analogues are described. Compounds were obtained in parallel combining solid phase and solution phase synthesis. The most active analogue is characterized by the octaclecyl group in position 2 of the glycerol chain. Considering that this substitution determines the loss of antitumor activity, a different mechanism of antileishmanial action can be hypothesized. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4658 / 4660
页数:3
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