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