Richard B Silverman and Mark W Holladay 

Academic Press

2014 | 536pp | £60.99

ISBN 9780123820303

The organic chemistry of drug design and drug action is a long-running textbook, first appearing over 20 years ago. This latest version has been updated to include a new co-author bringing greater industrial pharmaceutical experience to the text, as well as wider external input to strengthen the computational and QSAR (quantitative structure–activity relationship) components. 

The book covers the basic principles of drug design and action with a strong emphasis on the underlying organic chemistry processes. This is achieved with chapters covering the components of lead discovery, modification and optimisation as well as drug resistance, metabolism and delivery systems. 

For drug action, the material is presented in chapters on receptors and enzymes. The chapters are well constructed with clear examples, graphics and tables, as well as worked questions following each chapter, and would suit undergraduates at various stages of a chemistry degree. 

Focusing on the underlying principles rather than listing examples of drugs or drug targets works well, and although the chapter on enzymes goes into considerable detail on specific enzyme mechanisms, this strengthens the link from basic organic chemistry mechanisms to the understanding of key biochemical processes. Indeed, the emphasis on understanding the complexities of drug design and action from the fundamental principles of organic chemistry will be invaluable to those wishing to teach in this area without significant prior direct experience. 

From a personal perspective, the inclusion of a chapter entirely on DNA-interacting agents such as the intercalators and mustards and a large section on pro-drugs and delivery macromolecules overemphasises both topics in the context of teaching a new generation of chemists the principles of drug discovery. However, this does not detract from the value of the book overall. 

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