title: 5-Nitro-2-furyl derivative actives against Trypanosoma cruzi: preliminary in vivo studies.
abstract: Ten 5-nitro-2-furyl derivatives, with good to excellent in vitro anti-Trypanosoma cruzi activity, and nifurtimox were tested oral and intraperitoneally on healthy animals for its acute toxicity on murine models. According to animals' survival percentage, organ histological results, biochemical and haematological findings, three new derivatives, with toxicity like nifurtimox, were selected to test in vivo as antichagasic agents. Clearly, dependences between chemical structure and both acute toxicity and in vivo anti-T. cruzi activity were observed. 4-Hexyl-1-[3-(5-nitro-2-furyl)-2-propenylidene]semicarbazide displayed good profile as anti-T. cruzi agent and better acute toxicity profile than nifurtimox.
authors.affiliation: Departamento de Química Orgánica, Facultad de Química/Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
authors.forename: Eliana
authors.initials: E
authors.lastname: Cabrera
authors.forename: Mariana González
authors.initials: MG
authors.lastname: Murguiondo
authors.forename: Marelina González
authors.initials: MG
authors.lastname: Arias
authors.forename: Carolina
authors.initials: C
authors.lastname: Arredondo
authors.forename: Cristina
authors.initials: C
authors.lastname: Pintos
authors.forename: Gabriela
authors.initials: G
authors.lastname: Aguirre
authors.forename: Marcelo
authors.initials: M
authors.lastname: Fernández
authors.forename: Yester
authors.initials: Y
authors.lastname: Basmadjián
authors.forename: Raquel
authors.initials: R
authors.lastname: Rosa
authors.forename: José Pedro
authors.initials: JP
authors.lastname: Pacheco
authors.forename: Stella
authors.initials: S
authors.lastname: Raymondo
authors.forename: Rossanna
authors.initials: R
authors.lastname: Di Maio
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
mesh_terms: D000818:Animals; D014355:Chagas Disease / Q000188:drug therapy* / Q000473:pathology; D005260:Female; D051379:Mice; D009547:Nifurtimox / Q000737:chemistry* / Q000627:therapeutic use* / Q000633:toxicity; D009581:Nitrofurans / Q000737:chemistry* / Q000627:therapeutic use* / Q000633:toxicity; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000627:therapeutic use* / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D009581:Nitrofurans; D014344:Trypanocidal Agents; D009547:Nifurtimox