期刊
CURRENT MEDICINAL CHEMISTRY
卷 24, 期 6, 页码 622-651出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867323666161129124915
关键词
Urea; drug design; pharmacokinetics; enzyme inhibitors; epigenetics; intramolecular hydrogen binding
资金
- National Science Council (Ministry of Science and Technology) Taiwan
- National Taiwan University
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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