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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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Sanz AM,Gómez-Contreras F,Navarro P,Sánchez-Moreno M,Boutaleb-Charki S,Campuzano J,Pardo M,Osuna A,Cano C,Yunta MJ,Campayo L

doi

10.1021/jm701179m

subject

Has Abstract

pub_date

2008-03-27 00:00:00

pages

1962-6

issue

6

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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