Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 9, Pages 4231-4243Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm2017144
Keywords
-
Categories
Funding
- MCINN [CSD2010-00065, CTQ2009-14288-C04-01]
- FEDER
- Generalitat Valenciana PROMETEO
- Santander-Universidad Complutense Research [GR58/08-921371-891]
- Spanish MEC [CGL2008-03687-E/BOS]
Ask authors/readers for more resources
The in vitro and in vivo anti-Trypanosoma cruzi activity of the pyrazole-containing macrobicyclic polyamine 1 and N-methyl- and N-benzyl-substituted monocyclic polyamines 2 and 3 was studied. Activity against both the acute and chronic phases of Chagas disease was considered. The compounds were more active against the parasite and less toxic against Vero cells than the reference drug benznidazole, but 1 and 2 were especially effective, where cryptand 1 was the most active, particularly in the chronic phase. The activity results found for these compounds were complemented and discussed by considering their inhibitory effect on the iron superoxide dismutase enzyme of the parasite, the nature of the metabolites excreted after treatment, and the ultrastructural alterations produced. A complementary histopathological analysis confirmed that the compounds tested were significantly less toxic to mammals than the reference drug and that 1 and 2 exhibited lower levels of damage than 3.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available