ArticleJournal of medicinal chemistry2010
Identification and development of novel inhibitors of Toxoplasma gondii enoyl reductase.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 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
20 citing papers in PubMed, 50 citations in OpenAlex.
- Inhibitors of the FASII Metabolic Pathway inMicroorganisms · 2026Review
- Novel Scaffolds Based on Bis-thiazole Connected to Quinoxaline or Thienothiophene through 2-Phenoxy-ACS omega · 2023Article
- In Vitro Biological Activity of Natural Products from the Endophytic FungusAntibiotics (Basel, Switzerland) · 2022Article
- Building Programs to Eradicate Toxoplasmosis Part I: Introduction and Overview.Current pediatrics reports · 2022Review
- Building Programs to Eradicate Toxoplasmosis Part IV: Understanding and Development of Public Health Strategies and Advances "Take a Village".Current pediatrics reports · 2022Review
- A Systematic Review ofFrontiers in microbiology · 2017Review
- Clinically Available Medicines Demonstrating Anti-Toxoplasma Activity.Antimicrobial agents and chemotherapy · 2015Review
- Crystal structure of the human fatty acid synthase enoyl-acyl carrier protein-reductase domain complexed with triclosan reveals allosteric protein-protein interface inhibition.The Journal of biological chemistry · 2014Article
- Article
- Repurposing the open access malaria box to discover potent inhibitors of Toxoplasma gondii and Entamoeba histolytica.Antimicrobial agents and chemotherapy · 2014Article
- Anticancer, anti-inflammatory, and analgesic activities of synthesized 2-(substituted phenoxy) acetamide derivatives.BioMed research international · 2014Article
- Discrimination of potent inhibitors of Toxoplasma gondii enoyl-acyl carrier protein reductase by a thermal shift assay.Biochemistry · 2013Article
- Metabolic reconstruction identifies strain-specific regulation of virulence in Toxoplasma gondii.Molecular systems biology · 2013Article
- Modification of triclosan scaffold in search of improved inhibitors for enoyl-acyl carrier protein (ACP) reductase in Toxoplasma gondii.ChemMedChem · 2013Article
- Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides.Bioorganic & medicinal chemistry letters · 2013Article
- Design, synthesis, and biological activity of diaryl ether inhibitors of Toxoplasma gondii enoyl reductase.Bioorganic & medicinal chemistry letters · 2013Article
- Novel type II fatty acid biosynthesis (FAS II) inhibitors as multistage antimalarial agents.ChemMedChem · 2013Article
- Novel N-benzoyl-2-hydroxybenzamide disrupts unique parasite secretory pathway.Antimicrobial agents and chemotherapy · 2012Article
- Synthesis and biological evaluation of 2-(3-fluoro-4-nitro phenoxy)-n-phenylacetamide derivatives as novel potential affordable antitubercular agents.Molecules (Basel, Switzerland) · 2012Article
- Structure of the Yersinia pestis FabV enoyl-ACP reductase and its interaction with two 2-pyridone inhibitors.Structure (London, England : 1993) · 2012Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 1 country.
Funding
Abstract
Toxoplasmosis causes significant morbidity and mortality, and yet available medicines are limited by toxicities and hypersensitivity. Because improved medicines are needed urgently, rational approaches were used to identify novel lead compounds effective against Toxoplasma gondii enoyl reductase (TgENR), a type II fatty acid synthase enzyme essential in parasites but not present in animals. Fifty-three compounds, including three classes that inhibit ENRs, were tested. Six compounds have antiparasite MIC(90)s < or = 6 microM without toxicity to host cells, three compounds have IC(90)s < 45 nM against recombinant TgENR, and two protect mice. To further understand the mode of inhibition, the cocrystal structure of one of the most promising candidate compounds in complex with TgENR has been determined to 2.7 A. The crystal structure reveals that the aliphatic side chain of compound 19 occupies, as predicted, space made available by replacement of a bulky hydrophobic residue in homologous bacterial ENRs by Ala in TgENR. This provides a paradigm, conceptual foundation, reagents, and lead compounds for future rational development and discovery of improved inhibitors of T. gondii.
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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.