ABSTRACT
Until the 1970s, drug design was often a hit-and-miss affair where the emphasis was on synthesizing as many analogs of a lead compound as possible. Since, the emphasis has increasingly been on rational drug design based on an understanding of a drug’s mechanism of action and the structure of its target. Rational drug design is the norm rather than the exception and this change in emphasis has been due to advances in various scientific disciplines. Molecular biology has led to a much better understanding of the structure and function of important drug targets, such as enzymes and receptors. With an increase in life expectancy, the diseases of old age have become more significant, and research into novel drugs that can be used to treat Alzheimer’s disease, arthritis, and senility are of increasing importance. Important early example of rational drug design was the design and synthesis of the antihypertensive agents, captopril and enalapril.
