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There have been many changes in medicinal chemistry and molecular pharmacology since the second edition of this book was published in 1988. Accordingly, it has required extensive updating. This process was initiated in the Chemistry Department of Queen’s University, Kingston, Canada where Dr. Nico van Gelder, an Adjunct Emeritus Professor, introduced the now retired Thomas Nogrady to Donald Weaver, a medicinal chemist and clinical neurologist. Together, Weaver and Nogrady undertook the challenge of updating this book. In this way the third edition of Medicinal Chemistry was started and the two authors have worked together to ensure a continuity in the style and content that has made this book popular among students and researchers alike.
The areas of change in this new edition are many and varied. Since molecular modeling has assumed an increasingly prominent role in drug discovery, we have expanded the discussion of modeling techniques. Description of other new techniques such as high throughput screening and applications of genomics in drug design have also been added. In terms of medicinal chemistry applications, neuropharmacology has enjoyed many advances in the past decade; much new information from this field has been included.

In concert with these advances, new therapies have been introduced for Alzheimer’s disease, Parkinson’s disease, multiple sclerosis and epilepsy – these new therapies are explicitly discussed in the third edition. Emerging disorders like those of protein folding (e.g. Creutzfeldt-Jakob disease and other prion disorders) are also considered. Chapter 5 on hormonal therapies has been thoroughly updated and re-organized. An entire new chapter on the immune system has been added (chapter 6), reflecting the increased interest in therapeutic molecular manipulation of immunity. Emerging enzyme targets in drug design (e.g. kinases, caspases) are discusses in this edition.
Recent information on voltage-gated and ligand-gated ion channels has also been incorporated. The sections on antihypertensive, antiviral, antibacterial, anti-inflammatory, antiarrhythmic, and anti-cancer agents, as well as treatments for hyperlipidemia and for peptic ulcer, have been substantially expanded. Despite these many changes, the overall structure and philosophy of the book remain unchaged. Therapeutic agents are organized according to their targets – the conceptual centerpiece of the first two editions. The nine chapters of the third edition are grouped in two parts:

the basic principles of medicinal chemistry (chapters 1–3), and applications of medicinal chemistry from a target-centered viewpoint (chapters 4–9). Given this organizational structure, the book is not a catalogue of drugs. It does not present medicinal chemistry in a “telephone directory of drugs” way. Rather, it emphasizes the understanding of mechanisms of drug action, which includes drug and receptor structure. The book’s target-centered philosophy facilities a clear, mechanistic understanding of how and why drugs work. This should give students a conceptual framework that will enable them to continue learning about drugs and drug action long after they have left school.
As with the first and second editions, this text is aimed primarily at students of pharmacy, pharmacology and chemistry who are interested in drug design and development. It provides the core of biochemical- and molecular-level thinking about drugs needed for a basic medicinal chemistry course. Another new feature of this edition is designed to enhance the book’s appeal to all readers: the multiple sections on the “Clinical–Molecular Interface.” These sections strengthen the book’s clinical relevance by making it easier to understand the treatment of human disease at a molecular level.