Synthesis, analytical behaviour and biological evaluation of new 4-substituted pyrrolo[1,2-a]quinoxalines as antileishmanial agents |
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Authors: | Guillon Jean Forfar Isabelle Mamani-Matsuda Maria Desplat Vanessa Saliège Marion Thiolat Denis Massip Stéphane Tabourier Anais Léger Jean-Michel Dufaure Benoit Haumont Gilbert Jarry Christian Mossalayi Djavad |
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Affiliation: | EA 2962-Pharmacochimie, UFR des Sciences Pharmaceutiques, Université Victor Segalen Bordeaux 2, 146 rue Léo Saignat, 33076 Bordeaux Cedex, France. Jean.Guillon@chimphys.u-bordeaux2.fr |
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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. |
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