ArticleJournal of medicinal chemistry2011
Imidazolopiperazines: hit to lead optimization of new antimalarial agents.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
43 citing papers in PubMed.
- Safety, Pharmacokinetics, and Causal Prophylactic Efficacy of KAF156 in a Plasmodium falciparum Human Infection Study.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2021Trial
- A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine.Malaria journal · 2018Trial
- A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers.Antimicrobial agents and chemotherapy · 2014Trial
- A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel antimalarial Spiroindolone KAE609 (Cipargamin) to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers.Antimicrobial agents and chemotherapy · 2014Trial
- Drug Interaction Studies of Cabamiquine:Ganaplacide Combination against HepaticACS infectious diseases · 2025Article
- In-silico-based lead optimization of hit compounds targeting mitotic kinesin Eg5 for cancer management.In silico pharmacology · 2025Article
- Plasmodium SEY1 is a novel druggable target that contributes to imidazolopiperazine mechanism of action.Research square · 2024Article
- Applications of palladium-catalyzed C-N cross-coupling reactions in pharmaceutical compounds.RSC advances · 2023Review
- Solvent Moisture-Controlled Self-Assembly of Fused Benzoimidazopyrrolopyrazines with Different Ring's Interposition.Molecules (Basel, Switzerland) · 2022Article
- Therapeutic target database update 2022: facilitating drug discovery with enriched comparative data of targeted agents.Nucleic acids research · 2022Article
- A novel fungal metabolite inhibits Plasmodium falciparum transmission and infection.Parasites & vectors · 2021Article
- Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway inJournal of medicinal chemistry · 2021Article
- Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway.Nature communications · 2020Article
- Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials.ACS infectious diseases · 2020Article
- Synthesis and biological activities of local anesthetics.RSC advances · 2019Review
- The Groebke-Blackburn-Bienaymé Reaction.European journal of chemistry (Print) · 2019Article
- BIM-46174 fragments as potential ligands of G proteins.MedChemComm · 2019Article
- The genomic architecture of antimalarial drug resistance.Briefings in functional genomics · 2019Review
- Quantitative structure-activity relationship to predict the anti-malarial activity in a set of new imidazolopiperazines based on artificial neural networks.Malaria journal · 2019Article
- The past, present and future of anti-malarial medicines.Malaria journal · 2019Review
Corrections and comments
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Authors and funding
38 authors.
Funding
Abstract
Starting from a hit series from a GNF compound library collection and based on a cell-based proliferation assay of Plasmodium falciparum, a novel imidazolopiperazine scaffold was optimized. SAR for this series of compounds is discussed, focusing on optimization of cellular potency against wild-type and drug resistant parasites and improvement of physiochemical and pharmacokinetic properties. The lead compounds in this series showed good potencies in vitro and decent oral exposure levels in vivo. In a Plasmodium berghei mouse infection model, one lead compound lowered the parasitemia level by 99.4% after administration of 100 mg/kg single oral dose and prolonged mice survival by an average of 17.0 days. The lead compounds were also well-tolerated in the preliminary in vitro toxicity studies and represents an interesting lead for drug development.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.