title: Efficient inhibition of iron superoxide dismutase and of Trypanosoma cruzi growth by benzo[g]phthalazine derivatives functionalized with one or two imidazole rings.
abstract: The synthesis and trypanosomatic behavior of a new series of 1,4-bis(alkylamino)benzo[g]phthalazines 1- 4 containing the biologically significant imidazole ring are reported. In vitro antiparasitic activity against Trypanosoma cruzi epimastigotes is remarkable, especially for compound 2, whereas toxicity against Vero cells is very low. Conversion of epimastigotes to metacyclic forms in the presence of the tested compounds causes significant decreases in the amastigote and trypomastigote numbers. Fe-SOD inhibition is noteworthy, whereas effect on human Cu/Zn-SOD is negligible.
authors.affiliation: Departamento de Química Orgánica I, Facultad de Química, Universidad Complutense, Madrid, Spain.
authors.forename: Ana M
authors.initials: AM
authors.lastname: Sanz
authors.forename: Fernando
authors.initials: F
authors.lastname: Gómez-Contreras
authors.forename: Pilar
authors.initials: P
authors.lastname: Navarro
authors.forename: Manuel
authors.initials: M
authors.lastname: Sánchez-Moreno
authors.forename: Samira
authors.initials: S
authors.lastname: Boutaleb-Charki
authors.forename: Jose
authors.initials: J
authors.lastname: Campuzano
authors.forename: Mercedes
authors.initials: M
authors.lastname: Pardo
authors.forename: Antonio
authors.initials: A
authors.lastname: Osuna
authors.forename: Carmen
authors.initials: C
authors.lastname: Cano
authors.forename: María J R
authors.initials: MJ
authors.lastname: Yunta
authors.forename: Lucrecia
authors.initials: L
authors.lastname: Campayo
mesh_terms: D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D006801:Humans; D007093:Imidazoles / Q000737:chemistry*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010793:Phthalazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013482:Superoxide Dismutase / Q000037:antagonists & inhibitors*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development; D014709:Vero Cells / Q000187:drug effects
chemical_list: D000977:Antiparasitic Agents; D007093:Imidazoles; D010793:Phthalazines; D013482:Superoxide Dismutase