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Analogue-based Drug Discovery

Analogue-based Drug Discovery

IUPAC (Editor), János Fischer (Editor), C. Robin Ganellin (Editor)

ISBN: 978-3-527-60800-3

May 2006

606 pages

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.
Introduction
GENERAL ASPECTS OF ANALOGUE-BASED DRUG DISCOVERY
Analogues as a Means of Discovering New Drugs
Drug Likeness and Analogue-Based Drug Discovery
Privileged Structures and Analog-Based Drug Discovery
SELECTED EXAMPLES FROM THE ANALOGUE-BASED DRUG DISCOVERIES
Development of Anti-Ulcer H2-Receptor Histamine Antagonists
Esomeprazole in the Framework of Proton-Pump Inhibitor Development
The Development of a New Proton-Pump Inhibitor: The Case History of Pantoprazole
Optimizing the Clinical Pharmacologic Properties of the HMG-CoA Reductase Inhibitors
Optimizing Antihypertensive Therapy by Angiotensin Receptor Blockers
Optimizing Antihypertensive Therapy by Angiotensin-Converting Enzyme Inhibitors
Case Study of Lacidipine in the Research of New Calcium Antagonists
Selective Beta-Adrenergic Receptor-Blocking Agents
Case Study: ""Esmolol Stat"" [1]
Development of Organic Nitrates for Coronary Heart Disease
Development of Opioid Receptor Ligands
Stigmines
Structural Analogues of Clozapine
Quinolone Antibiotics: The Development of Moxifloxacin
The Development of Bisphosphonates as Drugs
Cisplatin and its Analogs for Cancer Chemotherapy
The History of Drospirenone
Histamine H1 Blockers: From Relative Failures to Blockbusters Within Series of Analogues
Corticosteroids: From Natural Products to Useful Analogues
""This book is eminently capable of educating both newcomers and experienced practitioners to the fields of medicinal chemistry and pharmacology, and it is highly recommended as an addition to the personal collection of the practicing drug designer and as a reference volume for institutional use as well.""
Journal of Medicinal Chemistry

""Overall the book is of interest for medicinal chemists who already have a sound knowledge of aspects of analogue-based drug design."" ChemMedChem