Wermuth / Aldous / Raboisson The Practice of Medicinal Chemistry

4. Auflage 2015
ISBN: 978-0-12-417213-5
Verlag: William Andrew Publishing
Format: EPUB
Kopierschutz: 6 - ePub Watermark

E-Book, Englisch, 902 Seiten, Format (B × H): 216 mm x 276 mm

The Practice of Medicinal Chemistry, Fourth Edition provides a practical and comprehensive overview of the daily issues facing pharmaceutical researchers and chemists. In addition to its thorough  treatment of basic medicinal chemistry principles, this updated edition has been revised to provide new and expanded coverage of the latest technologies and approaches in drug discovery.

With topics like high content screening, scoring, docking, binding free energy calculations, polypharmacology, QSAR, chemical collections and databases, and much more, this book is the go-to reference for all academic and pharmaceutical researchers who need a complete understanding of medicinal chemistry and its application to drug discovery and development.



- Includes updated and expanded material on systems biology, chemogenomics, computer-aided drug design, and other important recent advances in the field
- Incorporates extensive color figures, case studies, and practical examples to help users gain a further understanding of key concepts
- Provides high-quality content in a comprehensive manner, including contributions from international chapter authors to illustrate the global nature of medicinal chemistry and drug development research
- An image bank is available for instructors at www.textbooks.elsevier.com

Zielgruppe

<p>Pharmaceutical researchers and medicinal chemists involved in drug discovery in industry and academic settings, graduate-level students looking for a comprehensive reference on medicinal chemistry</p>

Autoren/Hrsg.

Wermuth, Camille Georges

Aldous, David

Raboisson, Pierre

Rognan, Didier

Fachgebiete

• Medizin | Veterinärmedizin Medizin | Public Health | Pharmazie | Zahnmedizin Pharmazie
• Naturwissenschaften Chemie Chemie Allgemein Pharmazeutische Chemie, Medizinische Chemie

Inhaltsverzeichnis

Section 1 - General Aspects of Medicinal Chemistry

Section 2 - Lead Compound Discovery Strategies

Section 3 - Primary Exploration of Structure-Activity Relationships

Section 4 - Substituents and Functions: Qualitative and Quantitative Aspects of Structure-Activity Relationships

Section 5 - Spatial Organization, Receptor Mapping and Molecular Modeling

Section 6 - Chemical Modifications Influencing the Pharmacokinetic Properties

Section 7 - Pharmaceutical and Chemical Means to Solubility and Formulation Problems

Leseproben

List of Contributors
Anne Badel,     UMR-S973, MTi, University Paris Diderot, Paris, France Patrick Bazzini,     PC SAS, Bd Gonthier d’Andernach, Illkirch, France Frans M. Belpaire,     Heymans Institute for Pharmacology, Gent, Belgium Alexandre Borrel University of Helsinki, Helsinki, Finland UMR-S973, MTi, University Paris Diderot, Paris, France Koen Boussery,     Laboratory of Medical Biochemistry and Clinical Analysis, Faculty of Pharmaceutical Sciences, Gent University, Gent, Belgium Christopher Brice,     Consultant, Luthi & Co., Intellectual Property Law Offices, of Tel Aviv, Israel Anne-Claude Camproux,     UMR-S973, MTi, University Paris Diderot, Paris, France David Cavalla,     Numedicus Ltd, Cambridge, England Paola Ciapetti,     Head of Medicinal Chemistry, Novalyst Discovery, Illkirch, Cedex, France Hongming Chen,     Chemistry Innovation Centre, Discovery Sciences, AstraZeneca R&D, Mölndal, Sweden Yong Mi Choi-Sledeski,     Sanofi, Boston, MA, USA Bernd Clement,     Pharmaceutical Institute, Christian Albrechts-University, Gutenbergstraße, Kiel, Germany Gordon M. Cragg,     NIH Special Volunteer, Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, United States National Cancer Institute, Frederick, Maryland, USA Patrick M. Dansette,     Laboratoire de Chimie et Biochimie Pharmacologique et Toxicologique, Université Paris Descartes, Sorbonne Paris Cité, Paris Pierre deMontigny,     Sanofi, Waltham, MA, U.S.A Ji-Cui Dong,     INN Programme, World Health Organization, Geneva Essential Medicines and Health Products, Regulation of Medicines and Other Health, Technologies, Technologies Standards and Norms Iain G. Dougall,     IGD Consultancy Ltd, Loughborough, Leics, UK Ola Engkvist,     Chemistry Innovation Centre, Discovery Sciences, AstraZeneca R&D, Mölndal, Sweden Bernard Faller,     Novartis Pharma AG, Werk Klybeck Klybeckstrasse, Basel, Switzerland Bennett T. Farmer,     Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT, USA Delphine Flatters,     UMR-S973, MTi, University Paris Diderot, Paris, France Bruno Galli,     Novartis Pharma AG, Lichtstrasse, Basel, Switzerland Colette Geneix,     UMR-S973, MTi, University Paris Diderot, Paris, France Bruno Giethlen,     Novartis Pharma AG, Basel, Switzerland Serge Grisoni,     Pierre Fabre Research Institute, Toulouse, Cédex, France Gerhard Gross,     Scientific Director at Janssen in Beerse, Belgium David Harris,     Sanofi, Waltham, MA, U.S.A Yuichi Hashimoto,     Institute of Molecular and Cellular Biosciences, The University of Tokyo, Japan Chris Ho,     Sanofi, Waltham, MA, U.S.A Andrew L. Hopkins,     College of Life Sciences, University of Dundee, Dundee, Scotland, UK Hiba Abi Hussein,     UMR-S973, MTi, University Paris Diderot, Paris, France Peter Imming,     Institut fuer Pharmazie, Martin-Luther-Universitaet Halle-Wittenberg, Halle, Germany Minoru Ishikawa,     Institute of Molecular and Cellular Biosciences, The University of Tokyo, Japan Tim Jonckers,     Janssen Research & Development Janssen Infectious Diseases – Diagnostics BVBA, Turnhoutseweg, Beerse, Belgium Sabine Kopp,     World Health Organization, Geneva Essential Medicines and Health Products, Regulation of Medicines and Other Health, Technologies, Technologies Standards and Norms David G.I. Kingston,     Department of Chemistry and the Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, Virginia, USA Thierry Kogej,     Chemistry Innovation Centre, Discovery Sciences, AstraZeneca R&D, Mölndal, Sweden Sophie Lasseur,     INN Programme, World Health Organization, Geneva Essential Medicines and Health Products, Regulation of Medicines and Other Health, Technologies, Technologies Standards and Norms Dominique Lesuisse,     Lead Generation Board, Sanofi, AVENUE PIERRE BROSSOLETTE, CHILLY MAZARIN - France Harvey Lieberman,     Sanofi, Waltham, MA, USA Richard Luthi,     Founding partner, Luthi & Co., Intellectual Property Law Offices, of Tel Aviv, Israel Anne-Christine Macherey,     Prévention du Risque Chimique, Gif sur Yvette, France André Mann,     LAAS-CNRS, Université Louis Pasteur, Strasbourg, France Raffaella G. Balocco Mattavelli,     INN Programme, World Health Organization, Geneva Essential Medicines and Health Products, Regulation of Medicines and Other Health, Technologies, Technologies Standards and Norms Christophe Morice,     Prestwick Chemical Inc., Boulevard Gonthier, Illkirch, France Richard Morphy,     Eli Lilly, Erl Wood Manor, Windlesham, Surrey, UK David J. Newman,     NIH Special Volunteer, Natural Products Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, United States National Cancer Institute, Frederick, Maryland, USA Anne Olivier,     Sanofi-Aventis Recherche et Développement, Chilly-Mazarin, France Michel Petitjean,     UMR-S973, MTi, University Paris Diderot, Paris, France Pierre Raboisson,     Janssen Infectious Diseases and Diagnostics BVBA, Beerse, Belgium Zoran Rankovic,     Eli Lilly, Indianapolis, IN, USA Leslie Regad,     UMR-S973, MTi, University Paris Diderot, Paris, France Allen B. Reitz,     Fox Chase Chemical Diversity Center, Inc., Doylestown, PA, USA Bernd U. Riebesehl,     Technical Research & Development, Novartis Pharma AG, Basel, Switzerland Jean-Philippe Rocher,     Pierre Fabre Research Institute, Castres, France Tiago Rodrigues,     Swiss Federal Institute of Technology (ETH), Department of Chemistry and Applied Biosciences, Zürich, Switzerland A. Romeo,     INN Programme, World Health Organization, Geneva Essential Medicines and Health Products, Regulation of Medicines and Other Health, Technologies, Technologies Standards and Norms Jean-Michel Rondeau,     Novartis Institutes for BioMedical Research, Basel, Switzerland Laurent Schaeffer,     Prestwick Chemical Inc., Boulevard Gonthier, Illkirch, France Jean-Michel Scherrmann,     Department of Pharmaceutical Sciences, University Paris...

Über Autor(innen)

Wermuth, Camille Georges
Camille-Georges Wermuth PhD, Prof. and Founder of Prestwick Chemical, was Professor of Organic Chemistry and Medicinal Chemistry at the Faculty of Pharmacy, Louis Pasteur University, Strasbourg, France from 1969 to 2002. He became interested in Medicinal Chemistry during his two years of military service in the French Navy at the "Centre d'Etudes Physio-biologiques Appliquées à la Marine" in Toulon. During this time he worked under the supervision of Dr Henri Laborit, the scientist who invented artificial hibernation and discovered chlorpromazine.

Professor Wermuths' main research themes focus on the chemistry and the pharmacology of pyridazine derivatives. The 3-aminopyridazine pharmacophore, in particular, allowed him to accede to an impressive variety of biological activities, including antidepressant and anticonvulsant molecules; inhibitors of enzymes such as mono-amine-oxidases, phosphodiesterases and acetylcholinesterase; ligands for neuro-receptors: GABA-A receptor antagonists, serotonine 5-HT3 receptor antagonists, dopaminergic and muscarinic agonists. More recently, in collaboration with the scientists of the Sanofi Company, he developed potent antagonists of the 41 amino-acid neuropeptide CRF (corticotrophin-releasing factor) which regulates the release of ACTH and thus the synthesis of corticoids in the adrenal glands. Professor Wermuth has also, in collaboration with Professor Jean-Charles Schwartz and Doctor Pierre Sokoloff (INSERM, Paris), developed selective ligands of the newly discovered dopamine D3 receptor. After a three-year exploratory phase, this research has led to nanomolar partial agonists which may prove useful in the treatment of the cocaine-withdrawal syndrome.

Dr. Wermuth is co-author or editor of several books, the author of over 250 scientific papers and holds nearly 60 patents. Professor Wermuth is also the recipient of the Charles Mentzer Prize of the Société Française de Chimie Thérapeutique, the Léon Velluz Prize of the French Academy of Science, the Prix de l'Ordre des Pharmaciens by the French Academy of Pharmacy and the Nauta Award of the European Federation for Medicinal Chemistry for Pharmacochemistry in 2010.