title: Synthesis, analytical behaviour and biological evaluation of new 4-substituted pyrrolo[1,2-a]quinoxalines as antileishmanial agents.
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.
authors.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
authors.forename: Jean
authors.initials: J
authors.lastname: Guillon
authors.forename: Isabelle
authors.initials: I
authors.lastname: Forfar
authors.forename: Maria
authors.initials: M
authors.lastname: Mamani-Matsuda
authors.forename: Vanessa
authors.initials: V
authors.lastname: Desplat
authors.forename: Marion
authors.initials: M
authors.lastname: Saliège
authors.forename: Denis
authors.initials: D
authors.lastname: Thiolat
authors.forename: Stéphane
authors.initials: S
authors.lastname: Massip
authors.forename: Anais
authors.initials: A
authors.lastname: Tabourier
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Léger
authors.forename: Benoit
authors.initials: B
authors.lastname: Dufaure
authors.forename: Gilbert
authors.initials: G
authors.lastname: Haumont
authors.forename: Christian
authors.initials: C
authors.lastname: Jarry
authors.forename: Djavad
authors.initials: D
authors.lastname: Mossalayi
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007891:Leishmania / Q000187:drug effects*; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D008958:Models, Molecular; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D011810:Quinoxalines