Analogue-based Drug Discovery
Published on 22. May 2006
Software
Other digital
606 pages
978-3-527-60800-3 (ISBN)
Description
The first authoritative overview of past and current strategies for successful drug development by analog generation, this unique resource spans all important drug classes and all major therapeutic fields, including histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds. Of the 19 analog classes presented in detail, 9 are described by the scientists who discoverd them. The book includes a table of the most successful drug analogs as based on the IMS ranking and compares them in terms of chemical structure, mode of action and patentability.
Reviews / Votes
"...eminently capable of educating both newcomers and experienced practitioners...highly recommended as an addition to the personal collection of the practicing drug designers and as a reference for institutional use..." (Journal of Medicinal Chemistry, July 27, 2006) "...will be welcomed by medicinal chemists...this well-produced book is fully referenced, and there is an extensive index." (Chemistry & Industry, April 2007)More details
Language
English
Place of publication
Weinheim
Germany
Target group
Professional and scholarly
Weight
10 gr
ISBN-13
978-3-527-60800-3 (9783527608003)
Copyright in bibliographic data and cover images is held by Nielsen Book Services Limited or by the publishers or by their respective licensors: all rights reserved.
Schweitzer Classification
Other editions
Additional editions
IUPAC | János Fischer | C. Robin Ganellin
Analogue-based Drug Discovery
E-Book
12/2006
1st Edition
Wiley-VCH
€234.99
Available for download
Person
Janos Fischer is research laboratory head at Richter Ltd. (Budapest, Hungary). He received his education in Hungary with B.Sc. and P.h. D. degrees in organic chemistry at the Eotvos University of Budapest with Professor A. Kucsman. Between 1976-78 he was a Humboldt fellow at the University of Bonn with Professor W. Steglich. He has worked at Richter Ltd. since 1981 where he participated in the research and development of leading cardiovascular drugs in Hungary. His main interest now is analog-based drug discovery. He is author of some 100 patents and scientific publications. In 2004 he was elected member of the Chemistry and Human Health Division of IUPAC. Robin Ganellin studied Chemistry at London University, receiving a PhD in 1958 under Professor Michael Dewar, and was a Research Associate at MIT with Arthur Cope in 1960. He then joined Smith Kline & French Laboratories in the UK and was one of the co-inventors of the revolutionary drug cimetidine (also known as Tagamet). In 1986 he was made a Fellow of the Royal Society and appointed to the SK&F Chair of Medicinal Chemistry at University College London, where he is now Emeritus Professor of Medicinal Chemistry. Professor Ganellin is co-inventor on over 160 patents and has authored 250 scientific publications. He was President of the Medicinal Chemistry Section of IUPAC and is currently Chairman of the IUPAC Subcommittee on Medicinal Chemistry and Drug Development.
Content
Preface.Introduction.List of Contributors.Abbreviations.PART I: GENERAL ASPECTS OF ANALOGUE-BASED DRUG DISCOVERY.1. Analogues as a Means of Discovering New Drugs.2. Drug Likeness and Analogue-Based Drug Discovery.3. Privileged Structures and Analog-Based Drug Discovery.PART II: SELECTED EXAMPLES FROM THE ANALOGUE-BASED DRUG DISCOVERIES.1. Development of Anti-Ulcer H2-Receptor Histamine Antagonists.2. Esomeprazole in the Framework of Proton-Pump Inhibitor Development.3. The Development of a New Proton-Pump Inhibitor: The Case History of Pantoprazole.4. Optimizing the Clinical Pharmacologic Properties of the HMG-CoA Reductase Inhibitors.5. Optimizing Antihypertensive Therapy by Angiotensin Receptor Blockers.6. Optimizing Antihypertensive Therapy by Angiotensin-Converting Enzyme Inhibitors.7. Case Study of Lacidipine in the Research of New Calcium Antagonists.8. Selective Beta-Adrenergic Receptor-Blocking Agents.9. Case Study: "Esmolol Stat".10. Development of Organic Nitrates for Coronary Heart Disease.11. Development of Opioid Receptor Ligands.12. Stigmines.13. Structural Analogues of Clozapine.14. Quinolone Antibiotics: The Development of Moxifloxacin.15. The Development of Bisphosphonates as Drugs.16. Cisplatin and its Analogs for Cancer Chemotherapy.17. The History of Drospirenone.18. Histamine H1 Blockers: From Relative Failures to Blockbusters Within Series of Analogues.19. Corticosteroids: From Natural Products to Useful Analogues.PART III: TABLE OF SELECTED ANALOGUE CLASSES.Index.