ArticleJournal of medicinal chemistry2012
Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 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
32 citing papers in PubMed.
- 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
- In vitro evaluation of ganaplacide/lumefantrine combination against Plasmodium falciparum in a context of artemisinin resistance.The Journal of antimicrobial chemotherapy · 2024Article
- Article
- Applications of palladium-catalyzed C-N cross-coupling reactions in pharmaceutical compounds.RSC advances · 2023Review
- Fast-Killing Tyrosine Amide ((ACS infectious diseases · 2023Article
- AssessmentAntimicrobial agents and chemotherapy · 2022Article
- Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway.Nature communications · 2020Article
- BIM-46174 fragments as potential ligands of G proteins.MedChemComm · 2019Article
- Quantitative structure-activity relationship to predict the anti-malarial activity in a set of new imidazolopiperazines based on artificial neural networks.Malaria journal · 2019Article
- Antiplasmodial Activity and In Vivo Bio-Distribution of Chloroquine Molecules Released with a 4-(4-Ethynylphenyl)-Triazole Moiety from Organometallo-Cobalamins.Molecules (Basel, Switzerland) · 2019Article
- The past, present and future of anti-malarial medicines.Malaria journal · 2019Review
- Plasmodium falciparum Cyclic Amine Resistance Locus (PfCARL), a Resistance Mechanism for Two Distinct Compound Classes.ACS infectious diseases · 2016Article
- Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.Chemical reviews · 2016Review
- UDP-galactose and acetyl-CoA transporters as Plasmodium multidrug resistance genes.Nature microbiology · 2016Article
- Phenotypic Screens in Antimalarial Drug Discovery.Trends in parasitology · 2016Review
- Article
- Inhibition of cytochrome bc1 as a strategy for single-dose, multi-stage antimalarial therapy.The American journal of tropical medicine and hygiene · 2015Article
- Review
Corrections and comments
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Authors and funding
31 authors.
Funding
Abstract
On the basis of the initial success of optimization of a novel series of imidazolopiperazines, a second generation of compounds involving changes in the core piperazine ring was synthesized to improve antimalarial properties. These changes were carried out to further improve the potency and metabolic stability of the compounds by leveraging the outcome of a set of in vitro metabolic identification studies. The optimized 8,8-dimethyl imidazolopiperazine analogues exhibited improved potency, in vitro metabolic stability profile and, as a result, enhanced oral exposure in vivo in mice. The optimized compounds were found to be more efficacious than the current antimalarials in a malaria mouse model. They exhibit moderate oral exposure in rat pharmacokinetic studies to achieve sufficient multiples of the oral exposure at the efficacious dose in toxicology studies.
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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.