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Ureas: Applications in Drug Design

[ Vol. 24 , Issue. 6 ]


Ajit Dhananjay Jagtap, Nagendra Bharatrao Kondekar, Amit A. Sadani and Ji-Wang Chern   Pages 622 - 651 ( 30 )


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.


Urea, drug design, pharmacokinetics, enzyme inhibitors, epigenetics, intramolecular hydrogen binding.


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

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