ArticleJournal of medicinal chemistry2014
Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP).
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 31 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.
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Who cites it
31 citing papers in PubMed, 76 citations in OpenAlex.
- Review
- Structure of Plasmodium vivaxN-myristoyltransferase with inhibitor IMP-1088: exploring an NMT inhibitor for antimalarial therapy.Acta crystallographica. Section F, Structural biology communications · 2025Article
- Ternary structure of Plasmodium vivaxN-myristoyltransferase with myristoyl-CoA and inhibitor IMP-0001173.Acta crystallographica. Section F, Structural biology communications · 2024Article
- Exploring Subsite Selectivity withinJournal of medicinal chemistry · 2024Article
- Identification of potent and selective N-myristoyltransferase inhibitors of Plasmodium vivax liver stage hypnozoites and schizonts.Nature communications · 2023Article
- Fungal Zinc Homeostasis and Its Potential as an Antifungal Target: A Focus on the Human PathogenMicroorganisms · 2022Review
- Phosphomannose Isomerase Is Involved in Development, Stress Responses, and Pathogenicity of Aspergillus flavus.Microbiology spectrum · 2022Article
- Molecular Characterization and the Essential Biological Function of the Metal Chaperone Protein MtmA in Aspergillus fumigatus.Applied and environmental microbiology · 2022Article
- Computer-aided identification of potential inhibitors againstInformatics in medicine unlocked · 2022Article
- Three-Component Synthesis of 2-Amino-3-cyano-4Pharmaceuticals (Basel, Switzerland) · 2021Article
- Inhibition of protein N-myristoylation blocks Plasmodium falciparum intraerythrocytic development, egress and invasion.PLoS biology · 2021Article
- Article
- Novel Thienopyrimidine Inhibitors ofJournal of medicinal chemistry · 2020Article
- Aspergillus fumigatus Mitochondrial Acetyl Coenzyme A Acetyltransferase as an Antifungal Target.Applied and environmental microbiology · 2020Article
- Structure-Guided Identification of Resistance Breaking Antimalarial N‑Myristoyltransferase Inhibitors.Cell chemical biology · 2019Article
- A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors.Journal of medicinal chemistry · 2018Article
- Increasing the Strength and Production of Artemisinin and Its Derivatives.Molecules (Basel, Switzerland) · 2018Review
- Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners.Molecules (Basel, Switzerland) · 2017Article
- N-Myristoyltransferase Inhibition Induces ER-Stress, Cell Cycle Arrest, and Apoptosis in Cancer Cells.ACS chemical biology · 2016Article
- Drug target identification in protozoan parasites.Expert opinion on drug discovery · 2016Review
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
N-Myristoyltransferase (NMT) is an essential eukaryotic enzyme and an attractive drug target in parasitic infections such as malaria. We have previously reported that 2-(3-(piperidin-4-yloxy)benzo[b]thiophen-2-yl)-5-((1,3,5-trimethyl-1H-pyrazol-4-yl)methyl)-1,3,4-oxadiazole (34c) is a high affinity inhibitor of both Plasmodium falciparum and P. vivax NMT and displays activity in vivo against a rodent malaria model. Here we describe the discovery of 34c through optimization of a previously described series. Development, guided by targeting a ligand efficiency dependent lipophilicity (LELP) score of less than 10, yielded a 100-fold increase in enzyme affinity and a 100-fold drop in lipophilicity with the addition of only two heavy atoms. 34c was found to be equipotent on chloroquine-sensitive and -resistant cell lines and on both blood and liver stage forms of the parasite. These data further validate NMT as an exciting drug target in malaria and support 34c as an attractive tool for further optimization.
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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.