ArticleJournal of medicinal chemistry2014
Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed.
- Pyridyl-Imidazopyridine Derivatives Displaying Submicromolar Activity Against Trypanosoma cruzi.ChemMedChem · 2026Article
- Optimization of Species-Selective Reversible Proteasome Inhibitors for the Treatment of Malaria.Journal of medicinal chemistry · 2025Article
- Anti-Cryptosporidium efficacy of BKI-1708, an inhibitor of Cryptosporidium calcium-dependent protein kinase 1.PLoS neglected tropical diseases · 2025Article
- Highly Enantioselective Lewis Acid Catalyzed Conjugate Addition of Imidazo[1,2-The Journal of organic chemistry · 2024Article
- The proteasome as a drug target for treatment of parasitic diseases.Advances in parasitology · 2024Review
- Synthesis and Antiproliferative Activity of 2,6-Disubstituted Imidazo[4,5-Molecules (Basel, Switzerland) · 2023Article
- Optimization of Orally Bioavailable Antileishmanial 2,4,5-Trisubstituted Benzamides.Journal of medicinal chemistry · 2023Article
- Comparison of Toxicities among Different Bumped Kinase Inhibitor Analogs for Treatment of Cryptosporidiosis.Antimicrobial agents and chemotherapy · 2023Article
- High-Throughput Screening Platform To Identify Inhibitors of Protein Synthesis with Potential for the Treatment of Malaria.Antimicrobial agents and chemotherapy · 2022Article
- Past and future of trypanosomatids high-throughput phenotypic screening.Memorias do Instituto Oswaldo Cruz · 2022Article
- Early Stages of Drug Discovery in an Academic Institution and Involvement of Pharma for Advancing Promising Leads.ACS infectious diseases · 2021Article
- Pyrrolopyrimidine Bumped Kinase Inhibitors for the Treatment of Cryptosporidiosis.ACS infectious diseases · 2021Article
- Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.Journal of medicinal chemistry · 2021Article
- Synthesis and Structure-Activity Relationships of Imidazopyridine/Pyrimidine- and Furopyridine-Based Anti-infective Agents against Trypanosomiases.ChemMedChem · 2021Article
- Whole-Cell Phenotypic Screening of Medicines for Malaria Venture Pathogen Box Identifies Specific Inhibitors ofAntimicrobial agents and chemotherapy · 2020Article
- Phenotypic Drug Discovery for Human African Trypanosomiasis: A Powerful Approach.Tropical medicine and infectious disease · 2020Article
- Ubiquitination and the Proteasome as Drug Targets in Trypanosomatid Diseases.Frontiers in chemistry · 2020Review
- Pharmacokinetics and In Vivo Efficacy of Pyrazolopyrimidine, Pyrrolopyrimidine, and 5-Aminopyrazole-4-Carboxamide Bumped Kinase Inhibitors against Toxoplasmosis.The Journal of infectious diseases · 2019Article
- Development of 5-Aminopyrazole-4-carboxamide-based Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy.Journal of medicinal chemistry · 2019Article
- Article
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Authors and funding
18 authors.
Funding
Abstract
A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of human African trypanosomiasis, led to the identification of substituted 2-(3-aminophenyl)oxazolopyridines as a starting point for hit-to-lead medicinal chemistry. A total of 110 analogues were prepared, which led to the identification of 64, a substituted 2-(3-aminophenyl)imidazopyridine. This compound showed antiparasitic activity in vitro with an EC50 of 2 nM and displayed reasonable druglike properties when tested in a number of in vitro assays. The compound was orally bioavailable and displayed good plasma and brain exposure in mice. Compound 64 cured mice infected with Trypanosoma brucei when dosed orally down to 2.5 mg/kg. Given its potent antiparasitic properties and its ease of synthesis, compound 64 represents a new lead for the development of drugs to treat human African trypanosomiasis.
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Registered trials
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