Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters











Database
Language
Publication year range
1.
J Med Chem ; 57(10): 3984-99, 2014 May 22.
Article in English | MEDLINE | ID: mdl-24749923

ABSTRACT

Chagas disease, caused by Trypanosoma cruzi parasite, was described thousands of years ago. Currently, it affects millions of people, mostly in Latin America, and there are not suitable drugs for treating it. As an attempt to find appropriate drugs to deal with this problem, we report here on the design, synthesis, and characterization of 82 new compounds. Trypanosomicidal behavior in vitro showed more than 20 outstanding derivatives with anti-Trypanosoma cruzi activity. Furthermore, we studied the nonspecific toxicity against mammalian cells determining their selectivity and also performed mutagenicity studies. Proof of concept, in vivo studies, was conducted with two of the most promising derivatives (77 and 80). They were identified as candidates because they have (i) very simple and cost-effective syntheses; (ii) activity against different stages and strains of the parasite showing excellent in vivo behavior during the acute phase of Chagas disease; and (iii) neither nonspecific toxicity nor mutagenic activity.


Subject(s)
Trypanocidal Agents/chemical synthesis , Trypanosoma cruzi/drug effects , Animals , Drug Stability , Female , Mice , Mice, Inbred BALB C , Mutation , Trypanocidal Agents/pharmacology , Trypanocidal Agents/toxicity
SELECTION OF CITATIONS
SEARCH DETAIL