The Symbiotic Relationship Between Drug Discovery and Organic Chemistry

All pharmaceutical products contain organic molecules; the source may be a natural product or a fully synthetic molecule, or a combination of both. Thus, it follows that organic chemistry underpins both existing and upcoming pharmaceutical products. The reverse relationship has also affected organic synthesis, changing its landscape towards increasingly complex targets. This Review article sets out to give a concise appraisal of this symbiotic relationship between organic chemistry and drug discovery, along with a discussion of the design concepts and highlighting key milestones along the journey. In particular, criteria for a high‐quality compound library design enabling efficient virtual navigation of chemical space, as well as rise and fall of concepts for its synthetic exploration (such as combinatorial chemistry; diversity‐, biology‐, lead‐, or fragment‐oriented syntheses; and DNA‐encoded libraries) are critically surveyed. Chemistry for drug discovery: All pharmaceutical products contain organic molecules, which may be sourced from natural products or be fully synthetic molecules. Thus, organic chemistry underpins both existing and upcoming pharmaceutical products. An appraisal of the relationship between synthetic chemistry and early drug discovery is given, along with a discussion on key concepts such as diversity‐, biology‐, and lead‐oriented syntheses (see figure).