ArticleInternational journal for parasitology. Drugs and drug resistance2022
Nucleoside analogues for the treatment of animal trypanosomiasis.
Article in International journal for parasitology. Drugs and drug resistance, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 21 citations in OpenAlex.
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- TargetingFrontiers in microbiology · 2026Review
- Guanine derivatives as promising candidates for the development of purine-based antimalarial drugs.Frontiers in parasitology · 2025Article
- Discovery of a Series of Macrocycles as Potent Inhibitors ofJournal of medicinal chemistry · 2024Article
- Drug resistance in animal trypanosomiases: Epidemiology, mechanisms and control strategies.International journal for parasitology. Drugs and drug resistance · 2024Review
- NParasitology · 2024Article
- Article
- Cloning and Characterization ofInternational journal of molecular sciences · 2023Article
- Pyrimidine salvage inFrontiers in cellular and infection microbiology · 2023Article
- Nucleoside Transport and Nucleobase Uptake Null Mutants inInternational journal of molecular sciences · 2022Article
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Animal trypanosomiasis (AT) is a parasitic disease with high socio-economic impact. Given the limited therapeutic options and problems of toxicity and drug resistance, this study assessed redirecting our previously identified antitrypanosomal nucleosides for the treatment of AT. Promising hits were identified with excellent in vitro activity across all important animal trypanosome species. Compound 7, an inosine analogue, and our previously described lead compound, 3'-deoxytubercidin (8), showed broad spectrum anti-AT activity, metabolic stability in the target host species and absence of toxicity, but with variable efficacy ranging from limited activity to full cure in mouse models of Trypanosoma congolense and T. vivax infection. Several compounds show promise against T. evansi (surra) and T. equiperdum (dourine). Given the preferred target product profile for a broad-spectrum compound against AT, this study emphasizes the need to include T. vivax in the screening cascade given its divergent susceptibility profile and provides a basis for lead optimization towards such broad spectrum anti-AT compound.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.