Perspectives in Drug Discovery

This chapter is intended to introduce readers to concepts and issues of medicinal chemistry. Three case histories are used to introduce the concept of bioisosteres; whether toxicities are caused by chemical structures or biologic mechanisms; the importance of selecting a preferred point of intervention in a disease process and selecting a biomarker to measure clinical efficacy; licensing a first-of-type compound for first to market and then modifying the structure for a preferred profile; and finally screening a series of compounds for efficacy, bioavailability and selectivity at the target site, ADME, and optimal formulations to select a preferred clinical candidate. Specific approaches to synthesis or high throughput screening are not covered in this introduction.