The synthetic modification of a biologically active compound, to fulfill stereo electronic, physicochemical, pharmacokinetic and toxicological clinical usefulness.
The process of creating the most advantageous lead drug compound, in terms of its biological activity, by refining its chemical and pharmacological properties.
The process of converting a putative lead compound ("hit") into a therapeutic drug with maximal activity and minimal side affects, typically using a combination of computer-based drug design, medicinal chemistry and pharmacology