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Related Experiment Videos

Progress in antischistosomal N,N'-diaryl urea SAR.

Jianbo Wu1, Chunkai Wang1, Derek Leas1

  • 1College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States.

Bioorganic & Medicinal Chemistry Letters
|January 11, 2018
PubMed
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New N,N-diaryl ureas show promise as antischistosomal drugs. Modifications improved solubility and maintained potent activity against Schistosoma mansoni, with some compounds demonstrating high plasma exposure and in vivo efficacy.

Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Drug Discovery

Background:

  • N,N'-Diaryl ureas represent a novel chemotype for antischistosomal drug development.
  • Schistosomiasis remains a significant global health concern, necessitating new therapeutic agents.

Purpose of the Study:

  • To design and synthesize novel N,N'-diaryl ureas with enhanced aqueous solubility and structural diversity.
  • To evaluate the physicochemical properties, in vitro ADME, plasma exposure, and antischistosomal activity of these new compounds.

Main Methods:

  • Synthesis of twenty new N,N'-diaryl ureas.
  • Physicochemical profiling, including lipophilicity and aqueous solubility assessment.
  • In vitro ADME studies, plasma exposure analysis, and ex vivo/in vivo activity testing against Schistosoma mansoni.
Keywords:
AntischistosomalN,N′-Diaryl ureaSAR

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Main Results:

  • Structural modifications, including replacement with azaheterocycles and benzoic acid derivatives, reduced lipophilicity and often increased aqueous solubility.
  • Compounds with 3-trifluoromethyl-4-pyridyl substructures exhibited metabolic stability.
  • Several N,N'-diaryl ureas demonstrated high ex vivo activity against S. mansoni with low cytotoxicity.
  • Compounds featuring 3-trifluoromethyl-4-pyridyl and 2,2-difluorobenzodioxole substructures showed the highest plasma exposures.
  • N,N'-diaryl ureas with 4-fluoro-3-trifluoromethylphenyl substructures displayed the best in vivo antischistosomal activity.

Conclusions:

  • The N,N'-diaryl urea scaffold can be chemically modified to improve physicochemical properties while retaining potent antischistosomal activity.
  • Specific structural features correlate with enhanced solubility, metabolic stability, plasma exposure, and in vivo efficacy.
  • Further development of these N,N'-diaryl ureas holds potential for new schistosomiasis treatments.