Today's top selling drugs have been uncovered from two major sources: natural products and laboratory synthesis. Those synthesised directly by medicinal chemists usually have been the result of a protracted discovery programme using a natural product (e.g. a hormone or an enzyme substrate) or a screening lead as a starting point. Many of the major categories of human disease cardiovascular, gastrointestinal, central nervous system, inflammatory and infectious diseases are included. After a short introduction to the discovery and mechanism of action of each drug, the syntheses of the best...