The Information is Available 11 Financial Considerations 11 Emergence of New Properties 12 Analogue Design as a Means of Discovering New Drugs 12 New Uses for Old Drugs 12 The PASS Program 14 New Leads from Old Drugs: The SOSA Approach 14 Definition 14 Rationale 15 Availability 15 Examples 15 Discussion 18 Conclusion 20ĭrug Likeness and Analogue-Based Drug Discovery 25 John R. Wermuthĭesigning of Analogues 3 Analogues Produced by Homologous Variations 3 Homology Through Monoalkylation 3 Polymethylenic Bis-Ammonium Compounds: Hexa- and Decamethonium 3 Homology in Cyclic Compounds 4 Analogues Produced by Vinylogy 4 Zaprinast Benzologues 5 Analogues Produced by Isosteric Variations 5 The Dominant Parameter is Structural 5 The Dominant Parameter is Electronic 6 The Dominant Parameter is Lipophilicity 7 Positional Isomers Produced as Analogues 7 Optical Isomers Produced as Analogues 8 Racemic Switches 8 Specific Profile for Each Enantiomer 8 Analogues Produced by Ring Transformations 9 Twin Drugs 9 The Pros and Cons of Analogue Design 10 The Success is Almost Warranted 10ġ.1.1.3 1.1.2 1.1.2.1 1.1.3 1.1.3.1 1.1.3.2 1.1.3.3 1.1.4 1.1.5 1.1.5.1 1.1.5.2 1.1.6 1.1.7 1.2 1.2.1ġ.2.2 1.2.3 1.2.4 1.3 1.3.1 1.3.2 1.3.3 1.3.3.1 1.3.3.2 1.3.3.3 1.3.3.4 1.3.3.4 1.4 General Aspects of Analogue-Based Drug Discovery 1Īnalogues as a Means of Discovering New Drugs 3 Camille G. Typesetting Kühn & Weyh, Satz und Medien, Freiburg Printing Strauss GmbH, Mörlenbach Bookbinding Schäffer GmbH, Gr ünstadt Cover-Design Grafik Design Schulz, Fußgönheim ISBN-13: ISBN-10: Printed in the Federal Republic of German y. used in this book, even when not specifically marked as such, are not to be considered unprotected by law. No part of this book may be reproduced in any form – nor transmitted or translated into machine language without written permission from the publishers.Registered names, trademarks, etc. KGaA, Weinheim All rights reserved (including those of translation into other languages). Bibliographic information published by Die Deutsche Bibliothek Die Deutsche Bibliothek lists this publication in the Deutsche Nationalbibliografie detailed bibliographic data is available in the Internet at. Library of Congress Card No.: applied for British Library Cataloguing-in-Publication Data A catalogue record for this book is available from the British Library. Readers are advised to keep in mind that statements, data, illustrations, procedural details or other items may inadvertently be inaccurate.
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Nevertheless, authors, editors, and publisher do not warrant the information contained in these books, including this book, to be free of errors. Robin Ganellin University College London Department of Chemistry 20 Gordon Street London WC1H OAJ UK Supported by The International Union of Pure and Applied Chemistry (IUPAC) Chemistry and Human Health Division PO Box 13757 Research Triangle Park, NC 27709-3757 USAĪll books published by Wiley-VCH are carefully produced. (eds.)Īnalgesics From Chemistry and Pharmacology to Clinical Application 2002, ISBN 3-7Įditors Dr. Pseudo-Peptides in Drug Discovery 2004, ISBN 3-1Ĭarbohydrate-based Drug Discovery 2003, ISBN 2-3īuschmann, H., Christoph, T., Friderichs, E., Maul, C., Sundermann, B. Pharmacophores and Pharmacophore Searches 2006, ISBN 0-1Ĭhemogenomics in Drug Discovery A Medicinal Chemistry Perspective 2004, ISBN 7-X Robin Ganellinįurther Titles of Interest Buschmann, H., Guitart, X., Torrens, A., Holenz, J., Quintana, J.Īntidepressants, Antipsychotics, Antianxiolytics From Chemistry and Pharmacology to Clinical Application 2006, ISBN 8-4 Robin GanellinĪnalogue-based Drug Discovery Edited by Já nos Fischer and C. Analogue-based Drug Discovery Edited by János Fischer and C.