Today I wanted to highlight books specifically on medicinal chemistry and drug discovery. Those are always festive additions to the holiday season, right? This list builds on last year’s recommendations, with updated editions of some titles, and adds a number of suggestions from readers.
I’ll start out with a recent history of our whole field: The Evolution of Drug Discovery. There are a lot of good books written at various levels about the discovery of particular drugs or therapies, but it’s rare to see the entire business of drug discovery looked at in this way.
For general medicinal chemistry, you have Bob Rydzewski’s Real World Drug Discovery: A Chemist’s Guide to Biotech and Pharmaceutical Research. A recent addition to this area is Drug Discovery: Practices, Processes, and Perspectives, by Jack Li and E. J. Corey. Another recommendation is Textbook of Drug Design and Discovery by Krogsgaard-Larsen et al. Several readers here have recommended earlier verions of Silverman’s medicinal chemistry book, and there’s now a third edition: The Organic Chemistry of Drug Design and Drug Action. Readers have also recommended Camille Wermuth’s The Practice of Medicinal Chemistry. For getting up to speed, several readers recommend Graham Patrick’s An Introduction to Medicinal Chemistry. Similarly, Medicinal Chemistry: The Modern Drug Discovery Process is a recent introductory textbook that I thought was well done.
Process chemistry is its own world with its own issues. Recommended texts here are Practical Process Research & Development by Neal Anderson, Repic’s Principles of Process Research and Chemical Development in the Pharmaceutical Industry, and Process Development: Fine Chemicals from Grams to Kilograms by Stan Lee (no, not that Stan Lee) and Graham Robinson. On an even larger scale, McConville’s The Pilot Plant Real Book comes recommended by readers here, too.
Another book that focuses on a particular (important) area of drug discovery is Robert Copeland’s Evaluation of Enzyme Inhibitors in Drug Discovery. Other recent books on particular areas of med-chem are Bioisosteres in Medicinal Chemistry by Brown et al., recommended by several readers, Scaffold Hopping in Medicinal Chemistry, and Protein-Protein Interactions in Drug Discovery, Volume 56
For chemists who want to brush up on their biology, readers recommended an earlier edition of this now updated Terrence Kenakin book: A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery , as well as Pharmacology in Drug Discovery: Understanding Drug Response. Cannon’s Pharmacology for Chemists, and Molecular Biology in Medicinal Chemistry by Nogrady and Weaver have also been recommended.
Overall, one of the most highly recommended books across the board comes from the PK end of things: Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization by Kerns and Di. This one is from 2008, but the same authors have another book coming out in February: Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs. Another recent PK-centric book is Lead Optimization for Medicinal Chemists. For getting up to speed in this area, there’s Pharmacokinetics Made Easy by Donald Birkett, and the Drug Metabolism and Pharmacokinetics Quick Guide has also been recommended.
In a related field, standard desk references for toxicology seems to be Casarett & Doull’s Toxicology: The Basic Science of Poisons and Hayes’ Principles and Methods of Toxicology Every medicinal chemist will end up learning a good amount toxicology, too often the hard way.
And a recently mentioned book here might prove useful as well: Navigating the Path to Industry, aimed at academic scientists (not just entry-level ones, either) who are looking at industrial research positions and wondering how to get from here to there.
As always, suggestions for more titles to add to the list are welcome.