Basic Concepts in Medicinal Chemistry

his book focuses solely on the basic, fundamental concepts governing the discipline of medicinal chemistry. Every drug is a chemical structure that contains numerous functional groups arranged in a specific manner. These functional groups determine the interactions of the drug molecule with its biological target, its pharmacological action, the route by which it is administered, the extent to which it is metabolized and the presence or absence of specific adverse reactions or drug interactions.

The chapters in this book have been carefully organized to allow the reader to gain knowledge progressively about the chemistry of drug molecules, with each chapter building on the previous one. The first chapter reviews the numbering of alicyclic and heterocyclic rings, the designation of aromatic ring positions and steroid nomenclature, while the second chapter focuses on the chemical characteristics of functional groups and the roles they play in drug action.

The following chapters identify those functional groups that are acidic or basic, review a strategy to calculate the extent to which they are ionised in a given environment and then examine how these characteristics contribute to the overall solubility of the drug molecule. Subsequent chapters discuss the types of binding interactions that can occur between a drug molecule and its biological target and how stereochemistry of the molecule can also affect its interaction with biological targets. Emphasis is placed on the pharmacological and therapeutic differences that can occur between enantiomers.

A chapter is devoted to exploring the metabolism of drug molecules by various enzymes. It identifies the functional groups that are susceptible to each type of metabolic transformation, enabling the reader to become more proficient in predicting the possible metabolic transformations for a given drug molecule. In the final chapter, the concept of structure-activity relationships is introduced along with the concepts of molecular modification to design new drugs and analogues of existing drugs. This book is extremely well structured and easy to follow. It navigates through medicinal chemistry in a way that makes the subject easy to understand. It will be a great asset to students embarking upon a healthcare career or to practitioners who need to brush up on medicinal chemistry.
(Laurence A. Goldberg Pharmaceutical Journal 2013-03-23)