- Synthesis, analytical behaviour and biological evaluation of new 4-substituted pyrrolo[1,2-a]quinoxalines as antileishmanial agents.
Synthesis, analytical behaviour and biological evaluation of new 4-substituted pyrrolo[1,2-a]quinoxalines as antileishmanial agents.
Bioorganic & medicinal chemistry (2006-10-20)
Jean Guillon, Isabelle Forfar, Maria Mamani-Matsuda, Vanessa Desplat, Marion Saliège, Denis Thiolat, Stéphane Massip, Anais Tabourier, Jean-Michel Léger, Benoit Dufaure, Gilbert Haumont, Christian Jarry, Djavad Mossalayi
PMID17049253
ABSTRACT
An original series of 4-substituted pyrrolo[1,2-a]quinoxaline derivatives, new structural analogues of Galipea species quinoline alkaloids, was synthesized from various substituted 2-nitroanilines via multistep heterocyclizations and tested for in vitro antiparasitic activity upon Leishmania amazonensis and Leishmania infantum strains. Structure-activity relationships enlighten the importance of the 4-substituted alkenyl side chain on the pyrrolo[1,2-a]quinoxaline moiety to modulate the antileishmanial activity.
MATERIALS