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Ureas: Applications in drug design

Research output: Contribution to journal › Review article › peer-review

Abstract

The unique hydrogen binding capabilities of ureas make them an important functional group to make drug-target interactions and thus incorporated in small molecules displaying broad range of bioactivities. The related research and numerous excellent achievements of ureas applicability in drug design for the modulation of selectivity, stability, toxicity and pharmacokinetic profile of lead molecules have become active topic. This review aims to provide insights in to the significance of urea in drug design by summarizing successful studies of various urea derivatives as modulators biological targets (viz. kinases, NAMPT, soluble epoxide hydrolases, mTOR, proteases, gyrB/parE, and epigenetic enzymes (such as HDAC, PRMT or DOT1L etc.). The findings of this review confirm the importance of urea moiety in medicinal chemistry and stimulate its use as a structural motif with rational decision making approach.

Original languageEnglish (US)
Pages (from-to)622-651
Number of pages30
JournalCurrent medicinal chemistry
Volume24
Issue number6
DOIs
StatePublished - Mar 1 2017
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2017 Bentham Science Publishers.

Keywords

  • Drug design
  • Enzyme inhibitors
  • Epigenetics
  • Intramolecular hydrogen binding
  • Pharmacokinetics
  • Urea

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