AI Article Synopsis
- Human African trypanosomiasis is a serious tropical disease that can be fatal without treatment, and current treatments have significant drawbacks like toxicity and limited effectiveness.
- A new compound, NEU-1053, has been discovered as a powerful and fast-acting treatment against the infection caused by Trypanosoma brucei in mouse models.
- Researchers are exploring variations of NEU-1053 to enhance its effectiveness and CNS exposure, and they are studying its effects and mechanisms through various methods, including X-ray crystallography.
Article Abstract
Human African trypanosomiasis is a neglected tropical disease that is lethal if left untreated. Existing therapeutics have limited efficacy and severe associated toxicities. 2-(2-(((3-((1H-Benzo[d]imidazol-2-yl)amino)propyl)amino)methyl)-4,6-dichloro-1H-indol-1-yl)ethan-1-ol (NEU-1053) has recently been identified from a high-throughput screen of >42,000 compounds as a highly potent and fast-acting trypanocidal agent capable of curing a bloodstream infection of Trypanosoma brucei in mice. We have designed a library of analogues to probe the structure-activity relationship and improve the predicted central nervous system (CNS) exposure of NEU-1053. We report the activity of these inhibitors of T. brucei, the efficacy of NEU-1053 in a murine CNS model of infection, and identification of the target of NEU-1053 via X-ray crystallography.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5346068 | PMC |
| http://dx.doi.org/10.1021/acsinfecdis.6b00202 | DOI Listing |
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