title: In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
abstract: 5-arylethenylbenzofuroxan derivatives with high in vitro anti-Trypanosoma cruzi activity were studied in vivo using acute murine models of Chagas' disease. The selected compounds, as pure isomeric forms, 1, 2, 3 and 4, or as equimolecular mixture of geometric isomers, 1:2, 3:4, 5:6 were studied against different T. cruzi strains. Consequently, Tulahuen 2 strain, Colombiana strain (resistant to Nifurtimox and Benznidazole), and two different wild strains, one isolated from the wild reservoir Didelphis marsupialis and another one from Uruguayan patients, were selected. No relevant signs of in vivo toxicity were observed with the benzofuroxans orally administered. Compound 1 and the mixture of isomers 1:2 were the best for treating infection against the four studied strains.
authors.affiliation: Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
authors.forename: Lucía
authors.initials: L
authors.lastname: Boiani
authors.forename: Carolina
authors.initials: C
authors.lastname: Davies
authors.forename: Carolina
authors.initials: C
authors.lastname: Arredondo
authors.forename: Williams
authors.initials: W
authors.lastname: Porcal
authors.forename: Alicia
authors.initials: A
authors.lastname: Merlino
authors.forename: Alejandra
authors.initials: A
authors.lastname: Gerpe
authors.forename: Mariana
authors.initials: M
authors.lastname: Boiani
authors.forename: José Pedro
authors.initials: JP
authors.lastname: Pacheco
authors.forename: Miguel Angel
authors.initials: MA
authors.lastname: Basombrío
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
mesh_terms: D000208:Acute Disease / Q000628:therapy; D000818:Animals; D000913:Antibodies, Protozoan / Q000378:metabolism; D001583:Benzoxazoles / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D014355:Chagas Disease / Q000188:drug therapy* / Q000276:immunology / Q000473:pathology / Q000628:therapy; D004195:Disease Models, Animal; D005260:Female; D051379:Mice; D018512:Parasitemia / Q000188:drug therapy; D016896:Treatment Outcome; D014349:Trypanosoma cruzi / Q000187:drug effects; D010069:Oxadiazoles
chemical_list: D000913:Antibodies, Protozoan; D001583:Benzoxazoles; C014354:benzofuroxan; D010069:Oxadiazoles