Ancient remedies find modern use

This book provides an introduction to the broad multi-disciplinary field of medicinal chemistry. The range of topics covered focuses on the chemical principles that underpin all aspects of drug discovery and design. It is primarily written for second and subsequent-year undergraduate degree courses in the fields of medicinal and pharmaceutical chemistry.

The introduction provides an historical perspective on how natural products have been used worldwide since ancient times for medicinal purposes. Paul Ehrlich's pioneering role during the early 1900s in developing a rational approach to designing novel chemotherapeutic agents is explained. Ehrlich's methods are then compared to current methodologies that include quantitative structure-activity relationships (QSAR), which led to the development of the antiulcer agents cimetidine and ranitidine.

The recurring theme of QSAR is illustrated by the development of drug groups such as the phenothiazine major tranquillisers and narcotic analgesics. Novel synthetic analogues, for example pethidine from morphine, or semi-synthetic analogues, such as penicillins, are described. The basic concepts of combinatorial chemistry are presented using the preparation of a hypothetical polyamine, describing both solid-phase and solution synthetic methods. Drug action on cell membranes, the importance of structure to the pharmacokinetic and metabolic fate of drugs, and species variability of drug response are detailed.

The section on enzymes (especially enzyme kinetics) is well explained, as is the mechanistic approach to explaining their catalytic activity. The transition state, and the importance of transition-state inhibitors is also described, as are receptor-ligand interactions. The role of nucleic acids, descriptions of DNA synthesis, transcription (to produce messenger-RNA) and translation (to produce proteins) are also well presented. This is a valuable and generally high-quality addition to the collection of introductory medicinal chemistry textbooks.

John E. Brown is senior lecturer in pharmaceutical chemistry, University of Bradford.