ArticleJournal of medicinal chemistry2019
Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis.
Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
What it found
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The trial behind it
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Who cites it
30 citing papers in PubMed, 28 citations in OpenAlex.
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- Myricetin InhibitsCells · 2026Article
- Functional characterization of 11 novel rhoptry proteins in the type I RH strain of Toxoplasma gondii using the CRISPR-Cas9 system.Parasites & vectors · 2026Article
- Biological Activity of Stilbenoids Against Fungal, Parasitic, and Viral Pathogens.Molecules (Basel, Switzerland) · 2026Review
- Discovery of quinazoline-based derivatives as novel autophagy inhibitors in pancreatic cancer.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- Therapeutic effect of baicalein as an antiparasitic agent againstJournal of Zhejiang University. Science. B · 2025Article
- Structure-Based Drug Design of Novel Heterocyclic Scaffolds as TgCDPK1 Inhibitors.ChemMedChem · 2025Article
- Protective Efficacy Induced by Virus-like Particles Expressing Dense Granule Protein 5 ofVaccines · 2025Article
- Molecular Detection of Genetic Material ofVeterinary sciences · 2025Article
- Biosensor Technology: Advances and Applications in Livestock Infectious Disease Diagnosis.Veterinary sciences · 2025Review
- Novel drug candidates targetingFrontiers in pharmacology · 2025Article
- Pharmacological validation of dihydrofolate reductase as a drug target inAntimicrobial agents and chemotherapy · 2024Article
- TaqMan-quantitative PCR assays applied inFrontiers in cellular and infection microbiology · 2024Article
- Sulfadiazine analogs: anti-Toxoplasma in vitro study of sulfonamide triazoles.Parasitology research · 2023Article
- Nanoformulation-Based 1,2,3-Triazole Sulfonamides for Anti-Tropical medicine and infectious disease · 2023Article
- Molecularly imprinted polymers (MIPs): emerging biomaterials for cancer theragnostic applications.Biomaterials research · 2023Review
- Computational screening of FDA-approved drugs to identify potential TgDHFR, TgPRS, and TgCDPK1 proteins inhibitors against Toxoplasma gondii.Scientific reports · 2023Article
- Design and synthesis of novel bis-pyridinium based-ionic liquids as potent antiparasitic agents.Heliyon · 2023Article
- TZD-Based Hybrid Molecules Act as Dual Anti-International journal of molecular sciences · 2023Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
Abstract
A safer treatment for toxoplasmosis would be achieved by improving the selectivity and potency of dihydrofolate reductase (DHFR) inhibitors, such as pyrimethamine (1), for Toxoplasma gondii DHFR ( TgDHFR) relative to human DHFR ( hDHFR). We previously reported on the identification of meta-biphenyl analog 2, designed by in silico modeling of key differences in the binding pocket between TgDHFR and hDHFR. Compound 2 improves TgDHFR selectivity 6.6-fold and potency 16-fold relative to 1. Here, we report on the optimization and structure-activity relationships of this arylpiperazine series leading to the discovery of 5-(4-(3-(2-methoxypyrimidin-5-yl)phenyl)piperazin-1-yl)pyrimidine-2,4-diamine 3. Compound 3 has a TgDHFR IC
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What OpenQuestion holds
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.