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.
Keywords: Urea, drug design, pharmacokinetics, enzyme inhibitors, epigenetics, intramolecular hydrogen binding.
Current Medicinal Chemistry
Title:Ureas: Applications in Drug Design
Volume: 24 Issue: 6
Author(s): Ajit Dhananjay Jagtap, Nagendra Bharatrao Kondekar, Amit A. Sadani and Ji-Wang Chern
Affiliation:
Keywords: Urea, drug design, pharmacokinetics, enzyme inhibitors, epigenetics, intramolecular hydrogen binding.
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.
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Cite this article as:
Jagtap Dhananjay Ajit, Kondekar Bharatrao Nagendra, Sadani A. Amit and Chern Ji-Wang, Ureas: Applications in Drug Design, Current Medicinal Chemistry 2017; 24 (6) . https://dx.doi.org/10.2174/0929867323666161129124915
DOI https://dx.doi.org/10.2174/0929867323666161129124915 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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