Patrick Paperback, 776 Pages 4th Edition, 2009 ISBN: 978-0-19-923447-9 Oxford University Press Description This lively, highly illustrated text provides undergraduate and postgraduate students with an accessible introduction to medicinal chemistry. It covers basic principles and background, and then describes the general tactics and strategies involved in developing an effective drug. Through the use of numerous examples it highlights both the difficulties faced by the medicinal chemist and the great potential of rational drug design. The second edition has five new chapters and is updated to include recent advances in the field. Editoral Review 'An Introduction to Medicinal Chemistry' clarifies the fundamentals of drug development with excellent examples and high quality graphics.
The book does not require extensive knowledge of biochemistry, but rather starts from scratch, covering the structure and function of enzymes and receptors, and the most important drug target structures. Illuminating explanations are given, such as that of the substantial role in protein structure played by van der Waals forces. The precise explanations of enzymes and receptors, and of the spectrum of possibilities between inhibition and excitation, convey the diversity of medicinal modes action. The actual drug design process is illustrated later on through the stages of development of specific drugs, in which the reader is provided with an overview of the modification options that elicit better binding to the target molecule.
The later chapters of 'An Introduction to Medicinal Chemistry' offer a many opportunities for more in-depth study. It is amazing how well-crafted explanations paired with appropriate graphics can enable a reader with essentially no background in biochemistry to become familiar with drug design. For this reason, this book can be recommended both beginning and advanced students, whether they envision a career in medicinal chemistry or are just pursuing an interest in this exciting field.
An Introduction to Medicinal Chemistry Patrick97397.indb i 9:11:41 PM This page intentionally left blank An Introduction to Medicinal Chemistry FIFTH EDITION Graham L. Patrick 1 Patrick97397.indb iii 9:11:45 PM 1 Great Clarendon Street, Oxford, OX2 6DP, United Kingdom Oxford University Press is a department of the University of Oxford. It furthers the University’s objective of excellence in research, scholarship, and education by publishing worldwide. Oxford is a registered trade mark of Oxford University Press in the UK and in certain other countries © Graham L. Patrick 2013 Th e moral rights of the author have been asserted Second Edition copyright 2001 Th ird Edition copyright 2005 Fourth Edition copyright 2009 Impression: 1 All rights reserved.
No part of this publication may be reproduced, stored in a retrieval system, or transmitted, in any form or by any means, without the prior permission in writing of Oxford University Press, or as expressly permitted by law, by licence or under terms agreed with the appropriate reprographics rights organization. Enquiries concerning reproduction outside the scope of the above should be sent to the Rights Department, Oxford University Press, at the address above You must not circulate this work in any other form and you must impose this same condition on any acquirer British Library Cataloguing in Publication Data Data available ISBN 978–0–19–969739–7 Printed in Italy by L.E.G.O. S.p.A.—Lavis TN Links to third party websites are provided by Oxford in good faith and for information only. Oxford disclaims any responsibility for the materials contained in any third party website referenced in this work. Patrick97397.indb iv 9:11:46 PM Preface Th is text is aimed at undergraduates and postgradu- ates who have a basic grounding in chemistry and are studying a module or degree in medicinal chemistry.
It attempts to convey, in a readable and interesting style, an understanding about drug design and the molecular mechanisms by which drugs act in the body. In so doing, it highlights the importance of medicinal chemistry in all our lives and the fascination of working in a fi eld which overlaps the disciplines of chemistry, biochemistry, physiology, microbiology, cell biology, and pharmacol- ogy. Consequently, the book is of particular interest to students who might be considering a future career in the pharmaceutical industry. New to this edition Following the success of the fi rst four editions, as well as useful feedback from readers, there has been some re o rganization and updating of chapters, especially those in Part E. Chapters have been modifi ed, as appropriate, to refl ect contemporary topics and teaching methods.
Th is includes:. new coverage of 99 drugs not featured in the previous edition;. six new boxes, covering topics such ‘Cyclodextrins as drug scavengers’, ‘Th e structure-based drug design of crizotinib’, and ‘Designing a non-steroidal glucocorti- coid agonist’;. a new case study on steroidal anti-infl ammatory agents;. over 25 new sections, providing additional depth in subject areas including ‘Tethers and anchors’ and ‘Short-acting β-blockers’;. additional end-of-chapter questions;.
current reference lists. We have also made signifi cant changes to the Online Resource Centre, adding 40 molecular modelling exer- cises and 16 web articles. The structure of the book Following the introductory chapter, the book is divided into fi ve parts. Part A contains six chapters that cover the structure and function of important drug targets, such as recep- tors, enzymes, and nucleic acids. Students with a strong background in biochemistry will already know this material, but may fi nd these chapters a useful revision of the essential points.
Part B covers pharmacodynamics in Chapters 7–10 and pharmacokinetics in Chapter 11. Pharmacody- namics is the study of how drugs interact with their molecular targets and the consequences of those interactions. Pharmacokinetics relates to the issues involved in a drug reaching its target in the fi rst place.
Part C covers the general principles and strategies involved in discovering and designing new drugs and developing them for the marketplace. Part D looks at particular ‘tools of the trade’ which are invaluable in drug design, i.e. QSAR, combinatorial synthesis, and computer-aided design. Part E covers a selection of specifi c topics within medicinal chemistry—antibacterial, antiviral and anti cancer agents, cholinergics and anticholinest- erases, adrenergics, opioid analgesics, and anti- ulcer agents. To some extent, those chapters refl ect the changing emphasis in medicinal chemistry research. Antibacterial agents, cholinergics, adren- ergics, and opioids have long histories and much of the early development of these drugs relied heav- ily on random variations of lead compounds on a trial and error basis.
Chemistry
Th is approach was waste- ful but it led to the recognition of various design strategies which could be used in a more rational approach to drug design. Th e development of the anti-ulcer drug cimetidine (Chapter 25) represents one of the early examples of the rational approach to medicinal chemistry. However, the real revolu- tion in drug design resulted from giant advances made in molecular biology and genetics which have provided a detailed understanding of drug targets and how they function at the molecular level. Th is, allied to the use of molecular modelling and X-ray crystallography, has revolutionized drug design. Convert pdf to word online free. Th e development of protease inhibitors as antiviral agents (Chapter 20), kinase inhibitors as anticancer agents (Chapter 21), and the statins as cholesterol- lowering agents (Case study 1) are prime examples of the modern approach. November 2012 Patrick97397.indb v 9:11:46 PM Emboldened key words Terminology is emboldened and defined in a glossary at the end of the book, helping you to become familiar with the language of medicinal chemistry. Boxes Boxes are used to present in-depth material and to explore how the concepts of medicinal chemistry are applied in practice.
Key points Summaries at the end of major sections within chapters highlight and summarize key concepts and provide a basis for revision. Questions End-of-chapter questions allow you to test your understanding and apply concepts presented in the chapter. Further reading Selected references allow you to easily research those topics that are of particular interest to you. Appendix The appendix includes an index of drug names and their corresponding trade names, and an extensive glossary. About the book present in the drug can be important in forming inter- molecular bonds with the target binding site.
If they do so, they are called binding groups. However, the carbon skeleton of the drug also plays an important role in bind- ing the drug to its target through van der Waals interac- tions. As far as the target binding site is concerned, it too contains functional groups and carbon skeletons which can form intermolecular bonds with ‘visiting’ drugs. The specific regions where this takes place are known as binding regions.
An Introduction To Medicinal Chemistry 5th Edition
The study of how drugs interact with their targets through binding interactions and produce a pharmacological effect is known as pharmacodynamics. One or more of the following interactions, but not neces- sarily all of them. 1.3.1 Electrostatic or ionic bonds An ionic or electrostatic.
Vintage drum machine samples. • Music created by established artists may be posted to ask specific production questions.
1.
2014-mastering-medicinal-chemistry-brochure.pdf - Worldwide Medicinal Chemistry, Pfizer, Inc. One drug design strategy for achieving pharmacological potency and selectivity. Medicinal Chemistry, AnalytiCon Discovery Download our introduction to medicinal chemistry 4th edition pdf eBooks for free and learn more about introduction to medicinal chemistry 4th edition pdf. These books contain exercises and tutorials to improve your practical skills, at all levels!
Bibliography Includes bibliographical references (p. 725-726) and index. Contents. 1. Drugs and drug targets: an overview- PART A: DRUG TARGETS: STRUCTURE AND FUNCTION- 2. Protein structure and function- 3. Enzymes: structure and function- 4.
Receptors: structure and function- 5. Receptors and signal transduction- 6. Nucleic acids: structure and function- PART B: PHARMACODYNAMICS AND PHARMACOKINETICS- 7. Enzymes as drug targets- 8.
Receptors as drug targets- 9. Nucleic acids as drug targets- 10. Other drug targets- 11. Pharmacokinetics and related topics- CASE STUDY 1: STATINS- PART C: DRUG DISCOVERY, DESIGN, AND DEVELOPMENT- 12. Drug discovery: finding a lead- 13.
Drug design: optimizing target interactions- 14. Drug design: optimizing access to the target- 15.
Getting the drug to market- CASE STUDY 2: THE DESIGN OF ACE INHIBITORS- CASE STUDY 3: ARTEMISININ AND RELATED ANTIMALARIAL DRUGS- CASE STUDY 4: THE DESIGN OF OXAMNIQUINE- PART D: TOOLS OF THE TRADE- 16. Combinatorial synthesis- 17. Computers in medicinal chemistry- 18. Quantitative structure-activity relationships (QSAR)- CASE STUDY 5: DE NOVO DESIGN OF A THYMIDYLATE SYNTHASE INHIBITOR- CASE STUDY 6: DESIGN OF A SEROTONIN ANTAGONIST AS A POSSIBLE ANXIOLYTIC AGENT- PART E: SELECTED TOPICS IN MEDICINAL CHEMISTRY- 19.
Antibacterial agents- 20. Antiviral agents- 21. Anticancer agents- 22. Cholinergics, anticholinergics, and anticholinesterases- 23. Drugs acting on the adrenergic nervous system- 24. The opium analgesics- 25.
Anti-ulcer agents- CASE STUDY 7: DESIGN OF A NOVEL ANTIDEPRESSANT. (source: Nielsen Book Data)48 Publisher's Summary The average person in the UK will take more than 14,000 pills over the course of their life, yet few people consider the long road of development that has made that drug work without being toxic. An Introduction to Medicinal Chemistry presents the field in an engaging style that is very accessible to students. Medicinal chemistry is a fast-moving field whose continuous new developments have far-reaching implications for world health.
As such, this text presents a complete course in medicinal chemistry, from first principles of drug action, to design and development, to specific drugs from HIV inhibitors to painkillers. The book builds on the history of drug development, but does not assume much background knowledge. The focus is on building upon the understandings of the molecular function of drugs, and from there, taking a broad overview of the topical issues and most frequently used techniques. An Introduction to Medicinal Chemistry remains a leading text for the growing number of medicinal chemistry courses internationally, especially as modules in medical chemistry become a more popular option on chemistry courses.With enhanced attention to the pedagogical details such as key points and boxes, as well as having specific case studies highlighted in distinct sections, Patrick's new edition enables a full understanding of the subject and a clear idea of where the field is heading.
Online Resource Centre The Online Resource Centre features: For registered adoptors of the book:. Answers to end-of-chapter questions.
Figures from the book. Power Point slides. Test Bank questions For students:. Hyperlinked bibliography. Six-monthly updates to text.
3D Rotatable structures. (source: Nielsen Book Data)48.
Patrick - An Introduction to Medicinal Chemistry, 4th Edition Oxford University Press 2009 ISBN: Pages: 752 DJVU 21.2 MB The average person in the UK will take more than 14,000 pills over the course of their life, yet few people consider the long road of development that has made that drug work without being toxic. An Introduction to Medicinal Chemistry presents the field in an engaging style that is very accessible to students. Medicinal chemistry is a fast-moving field whose continuous new developments have far-reaching implications for world health.
Medicinal Chemistry Journal
As such, this text presents a complete course in medicinal, from first principles of drug action, to design and development, to specific drugs from HIV inhibitors to painkillers. The book builds on the history of drug development, but does not assume much background knowledge. The focus is on building upon the understandings of the molecular function of drugs, and from there, taking a broad overview of the topical issues and most frequently used techniques.
An Introduction to Medicinal Chemistry remains a leading text for the growing number of medicinal chemistry courses internationally, especially as modules in medical chemistry become a more popular option on chemistry courses. With enhanced attention to the pedagogical details such as key points and boxes, as well as having specific case studies highlighted in distinct sections, Patrick's new edition enables a full understanding of the subject and a clear idea of where the field is heading.