Abstract
Methyl group is one of the most commonly occurring substituents in drugs. More than 50% of drugs with high market value have methyl groups in their structures. Methyl group has a capacity to act as Electron Donating Group and modulating physicochemical and biological properties of drug molecules. These properties include effect on half-life on a drug, selectivity, potency and binding affinity. When introduction of methyl group results in profound increase biological activity of molecules, it is known as Magic Methyl Effect. These enhancements in biological activity are attributed to effect of methyl group on free energy of Desolvation. The present review explores the origin of this magic methyl effect along with some supporting case studies in drug design.
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