ArticleJournal of medicinal chemistry2017
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
- Late-Stage Functionalization via Thianthrenation: A Reaction Enabling Rapid Preparation of Drug Beads for Chemical Pulldown.Journal of medicinal chemistry · 2026Article
- Identification and Evaluation of Dibasic Piperidines as Cell Wall Inhibitors againstACS infectious diseases · 2026Article
- Identification and Evaluation of dibasic piperidines as novel cell wall inhibitors againstbioRxiv : the preprint server for biology · 2026Article
- Structure-activity relationships of 1,5-dihydro-2RSC medicinal chemistry · 2025Article
- Aminopyridines in the development of drug candidates against protozoan neglected tropical diseases.Future medicinal chemistry · 2024Review
- A panel of phenotypically and genotypically diverse bioluminescent:fluorescent Trypanosoma cruzi strains as a resource for Chagas disease research.PLoS neglected tropical diseases · 2024Article
- Antitrypanosomal Activity of 1,2,3-Triazole-Based Hybrids Evaluated Using In Vitro Preclinical Translational Models.Biology · 2023Article
- Article
- Temporal and Wash-Out Studies Identify Medicines for Malaria Venture Pathogen Box Compounds with Fast-Acting Activity against BothMicroorganisms · 2022Article
- Synthesis and Anti-Molecules (Basel, Switzerland) · 2022Article
- Live-imaging rate-of-kill compound profiling for Chagas disease drug discovery with a new automated high-content assay.PLoS neglected tropical diseases · 2021Article
- Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with PotentJournal of medicinal chemistry · 2020Article
- Challenges in Chagas Disease Drug Development.Molecules (Basel, Switzerland) · 2020Review
- Nitrileimines as an alternative to azides in base-mediated click [3 + 2] cycloaddition with methylene active nitriles.RSC advances · 2020Article
- The QACS infectious diseases · 2020Article
- Hyperthermia Improves Solubility of Intravesical Chemotherapeutic Agents.Bladder cancer (Amsterdam, Netherlands) · 2020Article
- Flow Hydrodediazoniation of Aromatic Heterocycles.Molecules (Basel, Switzerland) · 2019Article
- 2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease.Bioorganic & medicinal chemistry letters · 2018Article
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Authors and funding
36 authors.
Funding
Abstract
Chagas' disease, caused by the protozoan parasite Trypanosoma cruzi, is the most common cause of cardiac-related deaths in endemic regions of Latin America. There is an urgent need for new safer treatments because current standard therapeutic options, benznidazole and nifurtimox, have significant side effects and are only effective in the acute phase of the infection with limited efficacy in the chronic phase. Phenotypic high content screening against the intracellular parasite in infected VERO cells was used to identify a novel hit series of 5-amino-1,2,3-triazole-4-carboxamides (ATC). Optimization of the ATC series gave improvements in potency, aqueous solubility, and metabolic stability, which combined to give significant improvements in oral exposure. Mitigation of a potential Ames and hERG liability ultimately led to two promising compounds, one of which demonstrated significant suppression of parasite burden in a mouse model of Chagas' disease.
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Registered trials
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