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Book Recommendations 2015: Medicinal Chemistry Books

So it’s true that they’re not everyone’s Christmas present, but I wanted to do my yearly roundup of books on medicinal chemistry and drug discovery. This list builds on last year’s recommendations, with updated editions of some titles, and adds a number of suggestions from readers.
A relatively recent (2011) history of our whole field is <The Evolution of Drug Discovery. There are many 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 covered like this.

For general medicinal chemistry, you have Bob Rydzewski’s Real World Drug Discovery: A Chemist’s Guide to Biotech and Pharmaceutical Research from 2008. And from 2013, there’s Drug Discovery: Practices, Processes, and Perspectives, by Jack Li and E. J. Corey. Another recommendation from several readers is Textbook of Drug Design and Discovery by Krogsgaard-Larsen et al. Several readers here have also recommended earlier versions of Silverman’s medicinal chemistry book, and now in its third edition: The Organic Chemistry of Drug Design and Drug Action. Readers have also recommended Camille Wermuth’s The Practice of Medicinal Chemistry, and it’s now in its fourth edition for 2015. Update: another one, just published in November, is Small Molecule Medicinal Chemistry: Strategies and Technologies. For getting up to speed, several readers recommend Graham Patrick’s An Introduction to Medicinal Chemistry (2013). Similarly, Medicinal Chemistry: The Modern Drug Discovery Process (Pearson Advanced Chemistry) is a recent introductory textbook that I found to be well written.

Process chemistry is its own world with its own issues. Recommended texts here are Practical Process Research and Development – A guide for Organic Chemists by Neal Anderson (2012). Repic’s Principles of Process Research and Chemical Development in the Pharmaceutical Industry is older (1998), but comes recommended as well. Another recommended text is Process Development: Fine Chemicals from Grams to Kilograms (Oxford Chemistry Primers) by Stan Lee (no, not that Stan Lee) and Graham Robinson. On an even larger scale, McConville’s The Pilot Plant Real Book is subtitled “A Unique Handbook”, and it comes recommended by readers here, too.

Case histories of successful past projects can be found in Drugs: From Discovery to Approval by Rick Ng, now in a new 2015 edition, and also in Walter Sneader’s Drug Discovery: A History. A recent addition to this area is Hallelujah Moments: Tales of Drug Discovery by longtime medicinal chemist Gene Cordes.

Another book that focuses on a particular (important) area of drug discovery is Robert Copeland’s Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists, and readers have specifically mentioned it as useful. Other recent books on particular areas of med-chem are Bioisosteres in Medicinal Chemistry, Volume 54 by Brown et al., recommended by several readers, Scaffold Hopping in Medicinal Chemistry, Prodrugs and Targeted Delivery: Towards Better ADME Properties, and Protein-Protein Interactions in Drug Discovery.

For chemists who want to brush up on their biology, readers recommended an earlier edition of this Terrence Kenakin book: A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, as well as his Pharmacology in Drug Discovery: Understanding Drug Response. Joseph Cannon’s Pharmacology for Chemistshas 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, which is the new edition coming out in early 2016. The same authors recently published Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs as well. Another recent PK-centric book is Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. For getting up to speed in this area, there’s Pocket Guide: Pharmacokinetics Made Easy (Pocket Guides) by Donald Birkett, which will not make all your pharmacokinetics problems easier, but will at least give you the tools to understand what’s going on, and the Drug Metabolism and Pharmacokinetics Quick Guide, which has also been recommended.

In a related field, standard textbooks for toxicology are Casarett & Doull’s Toxicology: The Basic Science of Poisons and Hayes’ Principles and Methods of Toxicology. A book on its application to drug development is Preclinical Safety Evaluation of Biopharmaceuticals: A Science-Based Approach to Facilitating Clinical Trials, from 2008.

Jerrold Zar’s Biostatistical Analysis comes recommended, and it’s a field that a lot of people (including me) could stand to be better at. For getting into this area, try Essential Biostatistics: A Nonmathematical Approach.

A book I reviewed last year might prove useful as well: Navigating the Path to Industry: A Hiring Manager’s Advice for Academics Looking for a Job in 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. Similarly, I very much enjoyed A Practical Guide to Drug Development in Academia, finding it full of very worthwhile advice for academic researchers looking to get into the pharma world with their own research.

10 comments on “Book Recommendations 2015: Medicinal Chemistry Books”

  1. Ash (Curious Wavefunction) says:

    I would like to add some popular titles to this excellent list:

    1. Mark Miodownik’s “Why Stuff Matters”.
    2. Keith Veronese’s “Rare: The High-Stakes Race to Satisfy Our Need for the Scarcest Metals on Earth”.
    3. Jonathan Waldman’s “Rust: The Longest War”.
    4. Robert Courland’s “Concrete Planet: The Strange and Fascinating Story of the World’s Most Common Man-Made Material”.
    5. Nick Lane’s “Oxygen: The molecule that made the world”.

    For case studies there’s also “Case Studies in Modern Drug Discovery and Development” by Xianhai Huang and Robert G. Aslanian.

    There’s also a great book on the chemistry of addiction (and an ACS publication to boot!) which I always recommend: Daniel Perrine’s “The Chemistry of Mind-Altering Drugs: History, Pharmacology, and Cultural Context”.

  2. Glad to see you spared me the need to plug Patrick again ;-). I have the latest edition of Kenakin ‘s primer and will vouch for it being terse in phrasing and a good overview of topics that won’t get a lot of coverage in academic chemistry programs. For people who feel out of their depth in statistics, Harvey Motulsky’s Intuitive Biostatistics is another great option. Motulsky is an MD who wrote the graphpad prism application and Intuitive Biostatistics is a hard-copy version of the theory documents that supported that program, rewritten for coherency. He favors explanations over derivations and avoids formulas where possible. It won’t prepare you for an advanced degree in statistics, but it is a thoroughly readable explanation of topics like p-values, statistical power, and confusion matricies. Easily enough to speak intelligently to any number-crunching professionals one encounters on the job.

    1. NJBiologist says:

      For the really math-averse, Motulsky has a new book called “Essential biostatistics: A nonmathematical approach” (Oxford University Press, about $20). The kid-based examples and XKCD strips target it to an audience just learning stats, but it’s a good book.

  3. NMH says:

    Im a biologist/biochemist that recently taught Org Chem at a PUI (It was tough!) Can anybody suggest to me a book about medicinal chemistry for biochem dolt like me so I can tell entertaining stories to a class about Med Chem in Org Chem, like, how it was one enatiomer of Thaliomide that caused all the birth defects? Thanks.

    1. Ivan Bushmarinov says:

      Any “entertaining story” in chemistry will still need a cross-check against the literature. For example, the enantiomers of thalidomide easily racemize in vivo, making the well-known tale you quoted particularly wrong.

  4. Guillermo Martinez Ariza says:

    Maybe I am biased because I contributed to one of the chapters but I think Small Molecule Medicinal Chemistry: Strategies and Technologies (Werngard Czechtizky, Peter Hamley editors) is a great book that was published online this year.

  5. Alex says:

    A complementary book to Patrick’s “An Introduction to Medicinal Chemistry” is also Patrick’s “An Introduction to Drug Synthesis” (OUP 2105)

  6. Chrispy says:

    As a graduate student in Organic Chemistry I found Robert Ireland’s Organic Synthesis from 1969 (!) fascinating. That was when I began to understand the real strategy behind synthesis and what made one synthesis elegant vs. another even if they both worked. These guys back then did not have the fancy reagents and tools we have now. If you like reading Woodward’s synthesis papers this book will be a winner for you, too.

  7. Sam Adams the Dog says:

    Can anyone suggest a book that gives good descriptions of the assays commonly used in early and late lead optimization? If one of the books mentioned in this thread, great; otherwise, another book or review article would be helpful.

    At this stage, I am less interested in the details of experimental method than I am in what the assays mean and when they are used.

    As examples, we have primary and secondary binding assays, human liver microsome clearance, CACO-2 permeability, log P, pKa, and so on.


  8. David Antonini says:

    Get Stan Lee to author or illustrate an accurate book on drug discovery, and you can bet the public’s understanding will increase!

    I’d buy it, anyway.

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