2. Academic Validation
  3. Efficient inhibition of iron superoxide dismutase and of Trypanosoma cruzi growth by benzo[g]phthalazine derivatives functionalized with one or two imidazole rings

Efficient inhibition of iron superoxide dismutase and of Trypanosoma cruzi growth by benzo[g]phthalazine derivatives functionalized with one or two imidazole rings

  • J Med Chem. 2008 Mar 27;51(6):1962-6. doi: 10.1021/jm701179m.
Ana M Sanz 1,  Fernando Gómez-Contreras,  Pilar Navarro,  Manuel Sánchez-Moreno,  Samira Boutaleb-Charki,  Jose Campuzano,  Mercedes Pardo,  Antonio Osuna,  Carmen Cano,  María J R Yunta,  Lucrecia Campayo
Affiliations

Affiliation

  • 1 Departamento de Química Orgánica I, Facultad de Química, Universidad Complutense, Madrid, Spain.
PMID: 18293910 DOI: 10.1021/jm701179m
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.

Figures