ArticleBioorganic & medicinal chemistry letters2018
Progress in antischistosomal N,N'-diaryl urea SAR.
Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 19 citations in OpenAlex.
- Structure-Activity Relationship of Antischistosomal Aryl Hydantoin (AR102).Journal of medicinal chemistry · 2025Article
- PfATP2 is a flippase on the Plasmodium falciparum surface that is important for growth and influences parasite sensitivity to antiplasmodial compounds.PLoS pathogens · 2025Article
- Synthesis of New N,N'-Diarylureas and Their Theoretical Study as Cannabinoid-1 Receptor Inhibitors.ChemPlusChem · 2025Article
- Article
- Diaryl Ureas as an Antiprotozoal Chemotype.ACS infectious diseases · 2021Article
- The Different Facets of Triclocarban: A Review.Molecules (Basel, Switzerland) · 2021Review
- Diarylureas: Repositioning from Antitumor to Antimicrobials or Multi-Target Agents against New Pandemics.Antibiotics (Basel, Switzerland) · 2021Review
- Schistosomiasis Drug Discovery in the Era of Automation and Artificial Intelligence.Frontiers in immunology · 2021Review
- Article
- Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?RSC medicinal chemistry · 2020Review
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Authors and funding
14 authors at 4 institutions in 3 countries.
Funding
Abstract
N,N'-Diaryl ureas have recently emerged as a new antischistosomal chemotype. We now describe physicochemical profiling, in vitro ADME, plasma exposure, and ex vivo and in vivo activities against Schistosoma mansoni for twenty new N,N'-diaryl ureas designed primarily to increase aqueous solubility, but also to maximize structural diversity. Replacement of one of the 4-fluoro-3-trifluoromethylphenyl substructures of lead N,N'-diaryl urea 1 with azaheterocycles and benzoic acids, benzamides, or benzonitriles decreased lipophilicity, and in most cases, increased aqueous solubility. There was no clear relationship between lipophilicity and metabolic stability, although all compounds with 3-trifluoromethyl-4-pyridyl substructures were metabolically stable. N,N'-diaryl ureas containing 4-fluoro-3-trifluoromethylphenyl, 3-trifluoromethyl-4-pyridyl, 2,2-difluorobenzodioxole, or 4-benzonitrile substructures had high activity against ex vivo S. mansoni and relatively low cytotoxicity. N,N-diaryl ureas with 3-trifluoromethyl-4-pyridyl and 2,2-difluorobenzodioxole substructures had the highest exposures whereas those with 4-fluoro-3-trifluoromethylphenyl substructures had the best in vivo antischistosomal activities. There was no direct correlation between compound exposure and in vivo activity.
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Registered trials
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