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J Med Chem ; 63(6): 3066-3089, 2020 03 26.
Article in English | MEDLINE | ID: mdl-32134269

ABSTRACT

Chagas disease is caused by the protozoan parasite Trypanosoma cruzi. It is endemic in South and Central America and recently has been found in other parts of the world, due to migration of chronically infected patients. The current treatment for Chagas disease is not satisfactory, and there is a need for new treatments. In this work, we describe the optimization of a hit compound resulting from the phenotypic screen of a library of compounds against T. cruzi. The compound series was optimized to the level where it had satisfactory pharmacokinetics to allow an efficacy study in a mouse model of Chagas disease. We were able to demonstrate efficacy in this model, although further work is required to improve the potency and selectivity of this series.


Subject(s)
Chagas Disease/drug therapy , Quinazolinones/therapeutic use , Trypanocidal Agents/therapeutic use , Trypanosoma cruzi/drug effects , Animals , Cell Line , Drug Discovery , Female , Mice, Inbred BALB C , Molecular Structure , Parasitic Sensitivity Tests , Proof of Concept Study , Quinazolinones/chemical synthesis , Quinazolinones/pharmacokinetics , Rats , Small Molecule Libraries/chemical synthesis , Small Molecule Libraries/pharmacokinetics , Small Molecule Libraries/therapeutic use , Structure-Activity Relationship , Trypanocidal Agents/chemical synthesis , Trypanocidal Agents/pharmacokinetics
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