Archived: The Magic Methyl in Medicinal Chemistry
Date: 29 April 2020
Commonly found in small molecule drugs, the humble methyl group can have a dramatic effect on binding affinity. A seemingly mundane change from C-H to C-Me can improve IC50 values by orders of magnitude. In addition methylation can have a favourable effect on solubility, off-target selectivity and has been used to introduce a ‘metabolic hotspot’ for shortening a persistent drugs half-life. Synthetic methods for direct activation and conversion of a C-H to C-Me, particularly in late stage functionalization of complex substrates, continues to be an active area of research in the synthetic community. These methods help drive innovation in medicinal and discovery chemistry.
Abracadabra! In this presentation we revealed some of the magic behind the methyl group, with examples and case studies, and explored state of the art enabling synthetic methodology.
This webinar was presented by Dr John Studley, Scientific Update and was kindly sponsored by Charnwood Molecular.