Medicinal Chemistry: An Introduction

Medicinal chemistry is the application of biology and chemistry to the design of new drugs for treating disease. It is the chemistry discipline concerned with the design, development and synthesis of pharmaceutical drugs. The discipline combines expertise from chemistry and pharmacology to identify, develop and synthesize chemical agents that have a therapeutic use and to evaluate the properties of existing drugs. Medicinal chemists apply their chemistry training to the process of synthesizing new pharmaceuticals. They also improve the processes by which existing pharmaceuticals are made. Medicinal chemists are focused on drug discovery and development and are concerned with the isolation of medicinal agents found in plants, as well as the creation of new synthetic drug compounds. Most chemists work with a team of scientists from different disciplines, including biologists, toxicologists, pharmacologists, theoretical chemists, microbiologists, and biopharmacists. Medicinal chemistry is a stimulating field as it links many scientific disciplines and allows for collaboration with other scientists in researching and developing new drugs. In particular, medicinal chemistry in its most common practice —focusing on small organic molecules—encompasses synthetic organic chemistry and aspects of natural products and computational chemistry in close combination with chemical biology, enzymology and structural biology, together aiming at the discovery and development of new therapeutic agents. Practically speaking, it involves chemical aspects of identification, and then systematic, thorough synthetic alteration of new chemical entities to make them suitable for therapeutic use. It includes synthetic and computational aspects of the study of existing drugs and agents in development in relation to their bioactivities, i.e., understanding their structure-activity relationships. Pharmaceutical chemistry is focused on quality aspects of medicines and aims to assure fitness for purpose of medicinal products. This book provides an introduction to medicinal chemistry. It covers basic principles and background, and describes the general tactics and strategies involved in effective drug design and development.