Advances in Medicinal Chemistry and Lead Optimization

Abstract

Abstract Medicinal chemistry applies both wet chemistry and computational methods to design, synthesize, and optimize the biological properties of compounds. An important phase of medicinal chemistry is lead optimization, a process whereby researchers design, synthesize, and retest analogues of primary lead compounds. During this process, medicinal chemists seek to identify compounds that are bioavailable and potent and that have high affinity and selectivity for their biological target. The goal of lead optimization is to find compounds that have acceptable pharmaceutical properties and can enter the next phases of drug development and clinical testing. In this article, we discuss advances in medicinal chemistry and its integration throughout drug discovery and early‐stage development, and we profile several companies specializing in this field.