LEADER 05293nam 2200673Ia 450 001 9911019809703321 005 20251116152151.0 010 $a9786610722761 010 $a9781280722769 010 $a1280722762 010 $a9783527608003 010 $a3527608001 010 $a9783527607495 010 $a3527607498 035 $a(CKB)1000000000376651 035 $a(EBL)481323 035 $a(SSID)ssj0000102851 035 $a(PQKBManifestationID)11109212 035 $a(PQKBTitleCode)TC0000102851 035 $a(PQKBWorkID)10060419 035 $a(PQKB)11714550 035 $a(MiAaPQ)EBC481323 035 $a(OCoLC)85821103 035 $a(Perlego)2750688 035 $a(EXLCZ)991000000000376651 100 $a20050620d2006 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aAnalogue-based drug discovery /$fJanos Fischer, C. Robin Ganellin 210 $aWeinheim ;$a[Chichester] $cWiley-VCH$dc2006 215 $a1 online resource (609 p.) 300 $aDescription based upon print version of record. 311 08$a9783527312573 311 08$a3527312579 320 $aIncludes bibliographical references and index. 327 $aAnalogue-based Drug Discovery; Contents; Preface; Introduction; List of Contributors; Abbreviations; Part I General Aspects of Analogue-Based Drug Discovery; 1 Analogues as a Means of Discovering New Drugs; 1.1 Designing of Analogues; 1.1.1 Analogues Produced by Homologous Variations; 1.1.1.1 Homology Through Monoalkylation; 1.1.1.2 Polymethylenic Bis-Ammonium Compounds: Hexa- and Decamethonium; 1.1.1.3 Homology in Cyclic Compounds; 1.1.2 Analogues Produced by Vinylogy; 1.1.2.1 Zaprinast Benzologues; 1.1.3 Analogues Produced by Isosteric Variations 327 $a1.1.3.1 The Dominant Parameter is Structural1.1.3.2 The Dominant Parameter is Electronic; 1.1.3.3 The Dominant Parameter is Lipophilicity; 1.1.4 Positional Isomers Produced as Analogues; 1.1.5 Optical Isomers Produced as Analogues; 1.1.5.1 Racemic Switches; 1.1.5.2 Specific Profile for Each Enantiomer; 1.1.6 Analogues Produced by Ring Transformations; 1.1.7 Twin Drugs; 1.2 The Pros and Cons of Analogue Design; 1.2.1 The Success is Almost Warranted; 1.2.2 The Information is Available; 1.2.3 Financial Considerations; 1.2.4 Emergence of New Properties 327 $a1.3 Analogue Design as a Means of Discovering New Drugs1.3.1 New Uses for Old Drugs; 1.3.2 The PASS Program; 1.3.3 New Leads from Old Drugs: The SOSA Approach; 1.3.3.1 Definition; 1.3.3.2 Rationale; 1.3.3.3 Availability; 1.3.3.4 Examples; 1.3.3.4 Discussion; 1.4 Conclusion; 2 Drug Likeness and Analogue-Based Drug Discovery; 3 Privileged Structures and Analogue-Based Drug Discovery; 3.1 Introduction; 3.2 Drugs from Side Effects; 3.3 Agonists and Antagonists; 3.4 Privileged Structures; 3.5 Drug Action on Target Classes; 3.5.1 GPCR Ligands; 3.5.2 Nuclear Receptor Ligands; 3.5.3 Integrin Ligands 327 $a3.5.4 Kinase Inhibitors3.5.5 Phosphodiesterase Inhibitors; 3.5.6 Neurotransmitter Uptake Inhibitors; 3.6 Summary and Conclusions; Part II Selected Examples of Analogue-Based Drug Discoveries; 1 Development of Anti-Ulcer H(2)-Receptor Histamine Antagonists; 1.1 Introduction; 1.2 The Prototype Drug, Burimamide, Defined Histamine H(2)-Receptors; 1.3 The Pioneer Drug, Cimetidine: A Breakthrough for Treating Peptic Ulcer Disease; 1.4 Ranitidine: The First Successful Analogue of H(2) Antagonists; 1.5 The Discovery of Tiotidine and Famotidine; 1.6 Other Compounds 327 $a1.7 The Use of H(2)-Receptor Histamine Antagonists as Medicines2 Esomeprazole in the Framework of Proton-Pump Inhibitor Development; 2.1 Towards Omeprazole: The First Proton-Pump Inhibitor; 2.2 The Treatment of Acid-Related Disorders Before LosecŪ; 2.3 Pioneer Research at Ha?ssle during the 1960s and 1970s; 2.3.1 Toxicological Challenges; 2.3.2 Discovery of H(+), K(+)-ATPase: The Gastric Proton Pump; 2.3.3 Analogue Optimization; 2.4 The Development of Omeprazole; 2.4.1 Further Toxicological Challenges and the Halt of the Clinical Program; 2.4.2 Resumption of Clinical Studies 327 $a2.4.3 Omeprazole Reaches the Market and Supersedes H(2)-Receptor Antagonists 330 $aThe 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 606 $aDrug development 606 $aPharmacology 615 0$aDrug development. 615 0$aPharmacology. 676 $a615.19 701 $aFischer$b Ja?nos$0881301 701 $aGanellin$b C. R$g(C. Robin)$0881302 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9911019809703321 996 $aAnalogue-based drug discovery$94422496 997 $aUNINA