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Ureas: Applications in Drug Design.

Ajit Dhananjay Jagtap, Nagendra Bharatrao Kondekar, Amit A Sadani

  • 1School of Pharmacy, and Center for Innovative Therapeutics Discovery, National Taiwan University, No. 33, Lin Sen South Road, Taipei 10050. Taiwan.

Current Medicinal Chemistry
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Summary

Urea functional groups are crucial in drug design due to their hydrogen binding abilities, enabling interactions with biological targets. This review highlights successful urea derivatives in modulating various targets, confirming their importance in medicinal chemistry.

Keywords:
Ureadrug designenzyme inhibitorsepigeneticsintramolecular hydrogen bindingpharmacokinetics

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Area of Science:

  • Medicinal Chemistry
  • Drug Design
  • Organic Chemistry

Background:

  • Ureas possess unique hydrogen binding capabilities, making them vital for drug-target interactions.
  • Their incorporation into small molecules leads to a broad range of bioactivities.
  • Urea derivatives have shown significant success in modulating drug properties like selectivity, stability, toxicity, and pharmacokinetics.

Purpose of the Study:

  • To review the significance of the urea moiety in drug design.
  • To summarize successful studies of urea derivatives as modulators of various biological targets.
  • To stimulate the rational use of urea as a structural motif in medicinal chemistry.

Main Methods:

  • Literature review of scientific studies on urea derivatives in drug design.
  • Summarization of research on urea's role in modulating specific biological targets.
  • Analysis of urea's impact on drug selectivity, stability, toxicity, and pharmacokinetic profiles.

Main Results:

  • Urea derivatives are effective modulators of diverse biological targets, including kinases, NAMPT, soluble epoxide hydrolases, mTOR, proteases, gyrB/parE, and epigenetic enzymes (HDAC, PRMT, DOT1L).
  • The urea functional group significantly influences drug properties, enhancing efficacy and safety.
  • Successful applications demonstrate the versatility of urea in developing novel therapeutics.

Conclusions:

  • The urea moiety is of paramount importance in medicinal chemistry and drug design.
  • Urea derivatives offer a promising structural motif for developing new drugs with improved therapeutic profiles.
  • Further research and rational design approaches utilizing urea are encouraged to advance drug discovery.