The Cyclopropyl Group in Medicinal Chemistry

The cyclopropane ring is now part of the established molecular architecture used in drug discovery and development, with a proven track record in marketed small molecule drugs. In total 18 NCE’s containing a cyclopropyl group were approved by the FDA over the past decade. There are several reasons this small ring system is attractive to drug hunters, including coplanarity of the three carbon atoms, shorter C-C bonds with enhanced p-character, and shorter C-H bonds that tend to be stronger than those in standard aliphatic chains. The cyclopropyl ring is often used as a isosteric replacement for an alkene or as a rigid alkyl linker and is also used strategically to increase potency, increase metabolic stability and reduce off-target effects.

This webinar looked in detail at the role of the cyclopropyl ring in drug discovery and development, including a review of the synthetic approaches used to install the cyclopropyl ring and/or key building blocks used in their assembly. Case-studies were used to draw out the key points, with examples from contemporary clinical molecules.

This webinar was presented by Dr John Studley, Scientific Update.