ArticleBioorganic & medicinal chemistry letters2013
Design, synthesis, and biological activity of diaryl ether inhibitors of Toxoplasma gondii enoyl reductase.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 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
10 citing papers in PubMed, 25 citations in OpenAlex.
- Inhibitors of the FASII Metabolic Pathway inMicroorganisms · 2026Review
- Lipid metabolism: the potential targets for toxoplasmosis treatment.Parasites & vectors · 2024Review
- The application of "plug-in molecules" method in novel strobilurin fungicides screening.RSC advances · 2020Article
- Drugs in development for toxoplasmosis: advances, challenges, and current status.Drug design, development and therapy · 2017Review
- Triazole-based compound as a candidate to develop novel medicines to treat toxoplasmosis.Antimicrobial agents and chemotherapy · 2014Article
- 1,4-Disubstituted thiosemicarbazide derivatives are potent inhibitors of Toxoplasma gondii proliferation.Molecules (Basel, Switzerland) · 2014Article
- The benzimidazole based drugs show good activity against T. gondii but poor activity against its proposed enoyl reductase enzyme target.Bioorganic & medicinal chemistry letters · 2014Article
- Discrimination of potent inhibitors of Toxoplasma gondii enoyl-acyl carrier protein reductase by a thermal shift assay.Biochemistry · 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
Corrections and comments
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Authors and funding
16 authors at 7 institutions in 2 countries.
Funding
Abstract
Triclosan is a potent inhibitor of Toxoplasma gondii enoyl reductase (TgENR), which is an essential enzyme for parasite survival. In view of triclosan's poor druggability, which limits its therapeutic use, a new set of B-ring modified analogs were designed to optimize its physico-chemical properties. These derivatives were synthesized and evaluated by in vitro assay and TgENR enzyme assay. Some analogs display improved solubility, permeability and a comparable MIC50 value to that of triclosan. Modeling of these inhibitors revealed the same overall binding mode with the enzyme as triclosan, but the B-ring modifications have additional interactions with the strongly conserved Asn130.
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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.