PREFACE This textbook provides a comprehensive set of basic notes in medicinal chemistry, which will be suit- able for undergraduate students studying a module in medicinal chemistry as part of a science, phar- macy or medical course. The book concentrates on the fundamental principles of medicinal chemi ind assumes no more than an elementary background of chemistry or biology It also serves as a useful first dipinto the subject for those students wishing to study medicinal chemistry itself Medicinal chemistry is an exciting new science, which has only come of age in the last 10-20 years It is a truly multidisciplinary subject involving such subject specialties as organic chemistry, pharma cology, biochemistry, physiology, microbiology, toxicology, genetics and computer modeling.Indeed most pharmaceutical companies organize research teams in such a way that scientists of different lisciplines interact with each other on a daily basis in order to fight the battle against disease. The very breadth of knowledge required by a medicinal chemist is both a challenge and a reward. Mastering an understanding of such a breadth of subject areas is no straightforward task, but by the same token there is ample intellectual stimulation in understanding the battle against disease at the molecular level and in designing molecular 'soldiers' to win that battle. This book attempts to condense the essentials of medicinal chemistry into a manageable text,which student friendly and does not cost an arm and a leg. It does this by concentrating purely on the basics of the subject without going into exhaustive detail or repetitive examples. Furthermore keynotes at the e Medicinal chemistry is a peculiar subject in that it feeds off so many other subjects. Understanding rt of each topic summarize the essential facts covered and help focus the mind on the essentials disease at the physiological, cellular and molecular levels is crucial if one is to design a suitable drug, and therefore knowledge of the relevant physiology, biochemistry, and pharmacology is of immense aid. However, the rapid advances made in two particular scientific areas are worth emphasizing Molecular biology and genetic engineering have produced a deluge of potential new targets for drug design and have unraveled the structures and mechanisms of traditional targets, while advances in computers and computer aided design have allowed medicinal chemists to take full advantage of thi newly earned knowledge Subsequent sections then follow the idenitabe n introduction to the science of medicinal chemistry The first four sections of this book serve stages that have to be negotiated by any date on its journey from initial brainstorm to the market place- a journey which takes many years and will see you graduated before it is! There are many difficult hurdles for the novice drug to over- come. The drug has to be ' so that it recognizes a specific target in the body and does not go fly- ingoffattacking' all and sundry. It has to gain access to the target by being absorbed into the blood upply, and in doing so it must be sturdy enough to ward off the many attacks that will be made on it by the bodys defenses. It must also be controlled in its'aggression', being a mild and harmless visitor during most of its body tour, but ruthless and efficient when it reaches its target. Designing such char acteristics is not: straightforward and a drugs behavior involves many tests and trials, both in the lab and in the clinic before it comes of age It is hoped that students will find this textbook useful in their studies and that once they have gra what medicinal chemistry is all about, they will read more widely and enter this truly exciting of molecular medicine