Discovery and Optimizationof a Compound Series Activeagainst Trypanosoma cruzi, the Causative Agent ofChagas Disease
2020
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.
Keywords:
- Correction
- Source
- Cite
- Save
- Machine Reading By IdeaReader
0
References
0
Citations
NaN
KQI