ArticleFrontiers in tropical diseases2023
Discovery of pyrazolopyrrolidinones as potent, broad-spectrum inhibitors of
Article in Frontiers in tropical diseases, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed, 8 citations in OpenAlex.
- Identification of natural products and synthetic analogs which inhibit microsporidia spores and prevent infection.Journal of invertebrate pathology · 2026Article
- Identification of Substituted 4-Aminocinnolines as Broad-Spectrum Antiparasitic Agents.ACS infectious diseases · 2025Article
- Insights into the Antiparasitic Activity of Pyrazole-benzimidazole againstCurrent medicinal chemistry · 2025Article
- Discovery and Optimization of Tambjamines as a Novel Class of Antileishmanial Agents.Journal of medicinal chemistry · 2024Article
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Authors and funding
15 authors at 7 institutions in 4 countries.
Funding
Abstract
Introduction: Leishmaniasis is a parasitic disease that affects more than 1 million people worldwide annually, predominantly in resource-limited settings. The challenge in compound development is to exhibit potent activity against the intracellular stage of the parasite (the stage present in the mammalian host) without harming the infected host cells. We have identified a compound series (pyrazolopyrrolidinones) active against the intracellular parasites of Methods: In this study, we performed medicinal chemistry on a newly discovered antileishmanial chemotype, with over 100 analogs tested. Studies included assessments of antileishmanial potency, toxicity towards host cells, and in vitro ADME screening of key drug properties. Results and discussion: Members of the series showed high potency against the deadliest form, visceral leishmaniasis (approximate EC Conclusion: Here, we describe preliminary structure-activity relationships for antileishmanial pyrazolopyrrolidinones, and our progress towards the identification of candidates for future in vivo assays in models of visceral and cutaneous leishmaniasis.
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