ArticleJournal of medicinal chemistry2019
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Xanthones and Their Nitrogen and Sulfur Analogs in Alzheimer's Disease: Recent Progress Toward Multifunctional Therapeutics.ChemMedChem · 2026Review
- Efficacy, Structure-Activity Relationship, and Mode of Action Studies of a New Generation of Acridine/Acridone-Based Antimalarials.ACS infectious diseases · 2026Article
- Evaluating acridones as novel therapeutics for human babesiosis.Antimicrobial agents and chemotherapy · 2026Article
- Potent acridone antimalarial against all three life stages of Plasmodium.Nature communications · 2026Article
- Optimization of Prodiginines as Single-Dose Curative Antimalarials.Journal of medicinal chemistry · 2025Article
- Acridone Prodrugs with Enhanced Dual-Stage Antimalarial Efficacy.ACS medicinal chemistry letters · 2025Article
- Development of Next-Generation Antimalarial Acridones with Radical Cure Potential.Journal of medicinal chemistry · 2025Article
- Structure-activity relationships ofExpert opinion on drug discovery · 2022Article
- Acridones Are Highly Potent Inhibitors ofACS infectious diseases · 2021Article
- Synthesis of novel cytotoxic tetracyclic acridone derivatives and study of their molecular docking, ADMET, QSAR, bioactivity and protein binding properties.Scientific reports · 2020Article
- Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.Journal of medicinal chemistry · 2020Article
- Boron Trifluoride Etherate Promoted Microwave-Assisted Synthesis of Antimalarial Acridones.RSC advances · 2019Article
Corrections and comments
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Authors and funding
39 authors.
Funding
Abstract
Malaria remains one of the deadliest diseases in the world today. Novel chemoprophylactic and chemotherapeutic antimalarials are needed to support the renewed eradication agenda. We have discovered a novel antimalarial acridone chemotype with dual-stage activity against both liver-stage and blood-stage malaria. Several lead compounds generated from structural optimization of a large library of novel acridones exhibit efficacy in the following systems: (1) picomolar inhibition of in vitro Plasmodium falciparum blood-stage growth against multidrug-resistant parasites; (2) curative efficacy after oral administration in an erythrocytic Plasmodium yoelii murine malaria model; (3) prevention of in vitro Plasmodium berghei sporozoite-induced development in human hepatocytes; and (4) protection of in vivo P. berghei sporozoite-induced infection in mice. This study offers the first account of liver-stage antimalarial activity in an acridone chemotype. Details of the design, chemistry, structure-activity relationships, safety, metabolic/pharmacokinetic studies, and mechanistic investigation are presented herein.
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