The cyclopropyl ring exhibits a number of interesting properties such as copolarity of the three carbon atoms, relatively short C-C and C-H bonds and enhanced π-characteristics of the C-C bonds. These allow the cyclopropyl moiety to bestow a range of beneficial effects on drug molecules which contain it. Some examples of this are: increased metabolic stability, enhanced potency, increased brain permeability and reduced off-target effects.
Other advantages include entropically more favourable binding to the receptor, and conformational restriction of peptides and peptidomimetrics to prevent proteolytic hydrolysis. This range of useful properties has led to the use of cyclopropyl-containing compounds in cardiovascular drugs, antidiabeticcs, autoimmune drugs, drugs for respiratory disorders, CNS active drugs, anti-cancer drugs, anti-virals and antibacterials.
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