Université Bordeaux Segalen, Pharmacochimie, CNRS, Pharmacochimie, FRE 3396, F-33000 Bordeaux, France.
Eur J Med Chem. 2011 Jun;46(6):2310-26. doi: 10.1016/j.ejmech.2011.03.014. Epub 2011 Mar 15.
Following our search for antimalarial compounds, novel series of ferrocenyl-substituted pyrrolo[1,2-a]quinoxalines 1-2 were synthesized from ferrocene-carboxaldehyde and tested for their in vitro activity upon the erythrocytic development of Plasmodium falciparum strains with different chloroquine-resistance status. The ferrocenic pyrrolo[1,2-a]quinoxalines 1-2 were prepared in 6 or 9 steps through a Barton-Zard reaction. Promising pharmacological results against FcB1, K1 and F32 strains were obtained with ferrocenyl pyrrolo[1,2-a]quinoxalines 1j-l linked by a bis-(3-aminopropyl)piperazine linker substituted by a nitrobenzyl moiety.
在我们寻找抗疟化合物的过程中，我们从二茂铁甲醛出发合成了一系列新型的二茂铁取代的吡咯并[1,2-a]喹喔啉 1-2，并对其在不同氯喹抗性状态的恶性疟原虫株的红细胞发育中的体外活性进行了测试。通过 Barton-Zard 反应，我们以 6 或 9 步的方式制备了二茂铁吡咯并[1,2-a]喹喔啉 1-2。带有硝基苄基取代基的双-(3-氨基丙基)哌嗪连接的二茂铁吡咯并[1,2-a]喹喔啉 1j-l 对 FcB1、K1 和 F32 菌株表现出有希望的药理活性。
