title: Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity.
abstract: We report the synthesis and in vitro activity against Trypanosoma cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 μM. Moreover, unspecific cytotoxicity and genotoxicity studies are also reported. Compound 14 showed a SI higher than 24, whereas compound 10 was the only one that was negative in the genotoxicity screening.
authors.affiliation: Department of Organic and Pharmaceutical Chemistry, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain; Institute of Tropical Health, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain.
authors.forename: Silvia
authors.initials: S
authors.lastname: Pérez-Silanes
authors.affiliation: Department of Organic and Pharmaceutical Chemistry, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain.
authors.forename: Enrique
authors.initials: E
authors.lastname: Torres
authors.affiliation: Department of Pharmacology and Toxicology, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain.
authors.forename: Leire
authors.initials: L
authors.lastname: Arbillaga
authors.affiliation: Grupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
authors.forename: Javier
authors.initials: J
authors.lastname: Varela
authors.affiliation: Grupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
authors.affiliation: Grupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
authors.affiliation: Department of Pharmacology and Toxicology, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain; IdiSNA, Navarra Institute for Health Research, Recinto de Complejo Hospitalario de Navarra c/Irunlarrea 3, Pamplona 31008, Spain.
authors.forename: Amaya
authors.initials: A
authors.lastname: Azqueta
authors.affiliation: Department of Organic and Pharmaceutical Chemistry, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain; Institute of Tropical Health, University of Navarra, Irunlarrea s/n, 31008 Pamplona, Spain. Electronic address: emviguri@unav.es.
authors.forename: Elsa
authors.initials: E
authors.lastname: Moreno-Viguri
mesh_terms: D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D009584:Nitrogen / Q000737:chemistry; D010087:Oxides / Q000737:chemistry; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects; D014709:Vero Cells
chemical_list: D010087:Oxides; D011810:Quinoxalines; D014344:Trypanocidal Agents; C003282:quindoxin; D009584:Nitrogen
keywords: Chagas disease; Cytotoxicity; Genotoxicity; Quinoxaline N-oxide; Trypanosoma cruzi