New ferrocenic pyrrolo[1,2-a]quinoxaline derivatives: Synthesis, and in vitro antimalarial activity – Part II
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- 作者：Jean Guillon ; Elisabeth Mouray ; Sté ; phane Moreau ; Catherine Mullié ; Isabelle Forfar ; Vanessa Desplat ; Solene Belisle-Fabre ; Noë ; l Pinaud ; Franç ; ois Ravanello ; Augustin Le-Naour ; Jean-Michel Lé ; ger ; Grace Gosmann ; Christian Jarry ; Gé ; rard Dé ; lé ; ris ; Pascal Sonnet ; Phi
- 关键词：Ferrocenic pyrrolo[1 ; 2-a]quinoxaline ; Antimalarial activity ; Plasmodium falciparum ; Synthesis
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2011
- 出版时间：June 2011
- 年：2011
- 卷：46
- 期：6
- 页码：2310-2326
- 全文大小：716 K
文摘
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.