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.
