ArticleACS medicinal chemistry letters2014
Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Plasmepsins as Antimalarial Drug Targets-Then, Now, and the Future.Medicinal research reviews · 2026Review
- Computational analysis of luteolin, apigenin and their derivatives from Allophylus africanus as potential inhibitors of plasmepsin II a malaria target.BMC chemistry · 2025Article
- Computer aided study on cyclic tetrapeptide based ligands as potential inhibitors of Proplasmepsin IV.Scientific reports · 2025Article
- Synthesis of β-fluoropyrrolidines designed to reduce hERG affinity in a class of antiparasitic compounds.ChemistrySelect · 2025Article
- Transmission-Blocking Strategies for Malaria Eradication: Recent Advances in Small-Molecule Drug Development.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Inhibition ofCurrent research in structural biology · 2024Article
- Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with PotentJournal of medicinal chemistry · 2023Article
- Substrate Peptidomimetic Inhibitors of P. falciparum Plasmepsin X with Potent Antimalarial Activity.ChemMedChem · 2022Article
- In pursuit of new anti-malarial candidates: novel synthesized and characterized pyrano-benzodioxepin analogues attenuatedHeliyon · 2021Article
- In vivo anti-malarial activity of the hydroalcoholic extract of rhizomes of Kniphofia foliosa and its constituents.Malaria journal · 2021Article
- Synthesis and Structure-Activity Relationships of N-(4-Benzamidino)-Oxazolidinones: Potent and Selective Inhibitors of Kallikrein-Related Peptidase 6.ChemMedChem · 2020Article
- 4-Aryl Pyrrolidines as a Novel Class of Orally Efficacious Antimalarial Agents. Part 1: Evaluation of 4-Aryl- N-benzylpyrrolidine-3-carboxamides.Journal of medicinal chemistry · 2019Article
- Structural Insights Into KeyFrontiers in microbiology · 2019Review
- Modeling and resistant alleles explain the selectivity of antimalarial compound 49c towards apicomplexan aspartyl proteases.The EMBO journal · 2018Article
- Alternatives to currently used antimalarial drugs: in search of a magic bullet.Infectious diseases of poverty · 2016Review
- Crystal structure of Plasmodium falciparum proplasmepsin IV: the plasticity of proplasmepsins.Acta crystallographica. Section F, Structural biology communications · 2016Article
- Structures of plasmepsin II from Plasmodium falciparum in complex with two hydroxyethylamine-based inhibitors.Acta crystallographica. Section F, Structural biology communications · 2015Article
- Malaria medicines: a glass half full?Nature reviews. Drug discovery · 2015Review
- Study of the antimalarial properties of hydroxyethylamine derivatives using green fluorescent protein transformed Plasmodium berghei.Memorias do Instituto Oswaldo Cruz · 2015Article
- Hydroxyethylamine Based Phthalimides as New Class of Plasmepsin Hits: Design, Synthesis and Antimalarial Evaluation.PloS one · 2015Article
Corrections and comments
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Authors and funding
12 authors.
Funding
Abstract
Antimalarial hit 1 SR (TCMDC-134674) identified in a GlaxoSmithKline cell based screening campaign was evaluated for inhibitory activity against the digestive vacuole plasmepsins (Plm I, II, and IV). It was found to be a potent Plm IV inhibitor with no selectivity over Cathepsin D. A cocrystal structure of 1 SR bound to Plm II was solved, providing structural insight for the design of more potent and selective analogues. Structure-guided optimization led to the identification of structurally simplified analogues 17 and 18 as low nanomolar inhibitors of both, plasmepsin Plm IV activity and P. falciparum growth in erythrocytes.
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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.