Journal
CHEMMEDCHEM
Volume 17, Issue 9, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202200020
Keywords
Cyclobutanes; strained carbocycles; conformational restriction; pharmacophores; isosteres
Categories
Funding
- Dutch Research Council (NWO) [189018]
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Cyclobutanes, with their unique structure, offer various benefits in medicinal chemistry, such as improving drug candidate properties through replacement of alkenes and larger cyclic systems.
Cyclobutanes are increasingly used in medicinal chemistry in the search for relevant biological properties. Important characteristics of the cyclobutane ring include its unique puckered structure, longer C-C bond lengths, increased C-C pi-character and relative chemical inertness for a highly strained carbocycle. This review will focus on contributions of cyclobutane rings in drug candidates to arrive at favorable properties. Cyclobutanes have been employed for improving multiple factors such as preventing cis/trans-isomerization by replacing alkenes, replacing larger cyclic systems, increasing metabolic stability, directing key pharmacophore groups, inducing conformational restriction, reducing planarity, as aryl isostere and filling hydrophobic pockets.
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