ArticleJournal of medicinal chemistry2014
Diversity-oriented synthesis-facilitated medicinal chemistry: toward the development of novel antimalarial agents.
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 17 papers.
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Who cites it
17 citing papers in PubMed.
- Repurposing sulfonamide-scaffolds for enhanced and sustainable malaria therapy.Future medicinal chemistry · 2025Review
- Article
- Mass spectrometry-based metabolomics uncovers distinct metabolic signatures and potential therapeutic targets in Plasmodium knowlesi.PloS one · 2025Article
- Innovations in Antimalarial Drug Discovery: New Targets and Leads.Current drug targets · 2025Review
- Ring Distortion of Vincamine Leads to the Identification of Re-Engineered Antiplasmodial Agents.ACS omega · 2021Article
- Pseudo Natural Products-Chemical Evolution of Natural Product Structure.Angewandte Chemie (International ed. in English) · 2021Review
- Re-Engineering of Yohimbine's Biological Activity through Ring Distortion: Identification and Structure-Activity Relationships of a New Class of Antiplasmodial Agents.ACS infectious diseases · 2020Article
- Recent Progress in the Development of New Antimalarial Drugs with Novel Targets.Drug design, development and therapy · 2020Review
- Antimalarial Drug Resistance and Novel Targets for Antimalarial Drug Discovery.Infection and drug resistance · 2020Review
- A Domino 10-Step Total Synthesis of FR252921 and Its Analogues, Complex Macrocyclic Immunosuppressants.Journal of the American Chemical Society · 2019Article
- Chemical probes and drug leads from advances in synthetic planning and methodology.Nature reviews. Drug discovery · 2018Review
- Targeting Channels and Transporters in Protozoan Parasite Infections.Frontiers in chemistry · 2018Review
- Modular Synthesis of Diverse Natural Product-Like Macrocycles: Discovery of Hits with Antimycobacterial Activity.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Article
- Modular, One-Pot, Sequential Aziridine Ring Opening-S(N)Ar Strategy to 7-, 10-, and 11-Membered Benzo-Fused Sultams.The Journal of organic chemistry · 2015Article
- Diversity-oriented synthesis probe targets Plasmodium falciparum cytochrome b ubiquinone reduction site and synergizes with oxidation site inhibitors.The Journal of infectious diseases · 2015Article
- Use of big data in drug development for precision medicine.Expert review of precision medicine and drug developmentArticle
Corrections and comments
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Authors and funding
22 authors.
Funding
Abstract
Here, we describe medicinal chemistry that was accelerated by a diversity-oriented synthesis (DOS) pathway, and in vivo studies of our previously reported macrocyclic antimalarial agent that derived from the synthetic pathway. Structure-activity relationships that focused on both appendage and skeletal features yielded a nanomolar inhibitor of P. falciparum asexual blood-stage growth with improved solubility and microsomal stability and reduced hERG binding. The build/couple/pair (B/C/P) synthetic strategy, used in the preparation of the original screening library, facilitated medicinal chemistry optimization of the antimalarial lead.
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Registered trials
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