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Vol. 35 No. 1
January-February 2013

Bookworm | Books and publications hot off the press.
See also www.iupac.org/publications

Analogue-based Drug Discovery III

Editors: Janos Fischer, C. Robin Ganellin, and David P. Rotella
Wiley-VCH, 2013, ISBN: 978-3-527-33073-7

“Analogue-based Drug Discovery” is the most general principle in medicinal chemistry. The analogue plays a very important role in both organic chemistry and pharmacology. A new compound is always compared to a reference compound, either from a chemical or biological viewpoint.

If referred to in such a general manner, then all medicinal chemistry should be included in the book Analogue-based Drug Discovery. However, our studies have been restricted to drugs that already have an existing reference drug. It has been investigated how new and better drugs could be obtained from already existing drug molecules.

The book series was developed with IUPAC support. The first volume (2006) mostly focused on structural and pharmacological analogues. Well-established drug classes have been studied from the viewpoint of drug optimization. The second volume (2010) had a broader scope, discussing several examples of pharmacological analogues. The third volume (2013) consists of three parts: General Aspects, Drug Classes, and Case Histories.

General Aspects

The introductory chapter discusses the relationship between pioneer and analogue drugs where their overlapping character can be observed. A chapter by Christian Tyrchan and Fabrizio Giordanetti (AstraZeneca) analyzes competition in pharmaceutical drug development. Amit S. Kalgutkar and Antonia F. Stepan (Pfizer) study the important role of metabolic stability in drug research. Mark L.Peterson, Hamit Hoveyda, Graeme Fraser, Éric Marsault, and René Gagnon (Tranzyme Pharma Inc.) write on the use of peptide-based macrocycles in drug design, exemplified by the discovery of ulimorelin.

Drug Classes

Arun Ganesan (University of East Anglia) gives an overview on discovery research into anticancer epigenetic drugs. Joseph A. Jakubowski (Lilly) and Atsushiro Sugidachi (Daiichi Sankyo) evaluate the structurally diverse drug class of the antithrombotic P2Y12 receptor antagonists. Paul Erhardt, Amarjit Luniwal, and Rachael Jetson (University of Toledo, USA) summarize the medicinal chemistry of selective estrogen receptor modulators. Kazumi Kondo and Hidenori Ogawa (Otsuka Phramaceutical Co., Japan) describe the discovery of aquaretics that are vasopressin V2 receptor antagonists. Peter R. Bernstein (PhaRmaB LLC) discusses the discovery of cysteinyl-leukotriene receptor antagonists, which are important in the treatment of asthma.

Part III (Case Histories)

Norbert Hauel, Andreas Clemens, Herbert Nar, Henning Priepke, Joanne vanRyn, and Wolfgang Wienen (Boehringer Ingelheim, Biberach, Germany) report on the discovery of dabigatran etexilate, an oral direct thrombin inhibitor approved for use in treatment of acute thrombosis. Klaus P. Bøgesø and Connie Sánchez (Lundbeck) descibe the discovery of escitalopram, which is one of the most successful selective serotonin reuptake inhibitors in the treatment of depressive disorders. Helmut Buschmann (Pharma-Consulting, Aachen, Germany) analyzes the discovery of tapentadol, a novel centrally acting synthetic analgesic with a dual mechanism of action. Hervé Bouchard, Drothée Semiond, Marie-Laure Risse, and Patricia Vrignaud (Sanofi) describe the discovery of cabazitaxel, a novel semisynthetic taxane, a new anticancer drug. Srikanth Venkatraman, Andrew Prongay, and George F. Njoroge (Merck) summarize the discovery of boceprevir and narlaprevir, hepatitis C protease inhibitors. Ken Okamoto, Shiro Kondo, and Takeshi Nishino (Nippon Medical School, Teijin Ltd and University of Tokyo) describe the discovery of febuxostat, a new uric-acid production inhibitor.

The book’s 15 chapters and 40 authors from 9 countries bring important, successful drug discoveries closer to medicinal chemists and all who are interested in the history of drug discoveries. The major part of the chapters are written by key inventors.

This book is the outcome of IUPAC project 2011-011-1-700.

www.iupac.org/project/2011-011-1-700

www.wiley.com


 

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