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The Organic Chemistry of Drug Design and Drug Action

Author: Richard B. Silverman

Publisher: Academic Press

ISBN:

Category: Medical

Page: 536

View: 171

The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition includes updates to all chapters, including new examples and references. It reflects significant changes in the process of drug design over the last decade and preserves the successful approach of the previous editions while including significant changes in format and coverage. This text is designed for undergraduate and graduate students in chemistry studying medicinal chemistry or pharmaceutical chemistry; research chemists and biochemists working in pharmaceutical and biotechnology industries. Updates to all chapters, including new examples and references Chapter 1 (Introduction): Completely rewritten and expanded as an overview of topics discussed in detail throughout the book Chapter 2 (Lead Discovery and Lead Modification): Sections on sources of compounds for screening including library collections, virtual screening, and computational methods, as well as hit-to-lead and scaffold hopping; expanded sections on sources of lead compounds, fragment-based lead discovery, and molecular graphics; and deemphasized solid-phase synthesis and combinatorial chemistry Chapter 3 (Receptors): Drug-receptor interactions, cation-π and halogen bonding; atropisomers; case history of the insomnia drug suvorexant Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug discovery and enzyme synthesis Chapter 5 (Enzyme Inhibition and Inactivation): New case histories: for competitive inhibition, the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor, imatinib for transition state analogue inhibition, the purine nucleoside phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the mechanism of the multisubstrate analog inhibitor isoniazid for slow, tight-binding inhibition, the dipeptidyl peptidase-4 inhibitor, saxagliptin Chapter 7 (Drug Resistance and Drug Synergism): This new chapter includes topics taken from two chapters in the previous edition, with many new examples Chapter 8 (Drug Metabolism): Discussions of toxicophores and reactive metabolites Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of antibody–drug conjugates

Textbook of Drug Design and Discovery, Third Edition

Author: Tommy Liljefors

Publisher: CRC Press

ISBN:

Category: Medical

Page: 592

View: 745

Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine. The book follows drug design from the initial lead identification through optimization and structure-activity relationship with reference to the final processes of clinical evaluation and registration. Chapters investigate the design of enzyme inhibitors and drugs for particular cellular targets such as ion channels and receptors, and also explore specific classes of drug such as peptidomimetics, antivirals and anticancer agents. The use of gene technology in pharmaceutical research, computer modeling techniques, and combinatorial approaches are also included.

The Organic Chemistry of Drug Design and Drug Action, Power PDF

Author: Richard B. Silverman

Publisher: Elsevier

ISBN:

Category: Medical

Page: 1275

View: 628

This CD-ROM edition of Silverman's Organic Chemisry of Drug Design and Drug Action, Second Edition reflects the significant changes in the drug industry in recent years, using an accessible interactive approach. This CD-ROM integrates the author's own PowerPoint slides, indexed and linked to the book pages in PDF format. The three-part structure includes an all-electronic text with full-text search capabilites and nearly 800 powerpoint slides. This is a unique and powerful combination of electronic study guide and full book pages. Users can hyperlink seamlessly from the main text to key points and figures on the outline and back again. It serves as a wonderful supplement for instructors as well as a fully integrated text and study aid for students. * Three-part package includes 1) powerpoint, 2) integrated powerpoint and pdf-based text, and 3) fully searchable PDF-based text with index * Includes new full-color illustrations, structures, schemes, and figures as well as extensive chapter problems and exercises * User-friendly buttons transition from overview (study-guide) format to corresponding book page and back with the click of a mouse * Full-text search capabality an incomparable tool for researchers seeking specific references and/or unindexed phrases

Medicinal Chemistry of Anticancer Drugs

Author: Carmen Avendano

Publisher: Elsevier

ISBN:

Category: Medical

Page: 400

View: 260

Antitumor chemotherapy is nowadays a very active field of research, and a huge amount of information on the topic is generated every year. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book addresses the need for an updated treatment from the point of view of medicinal chemistry and drug design. The focus of Medicinal Chemistry of Anticancer Drugs is on the mechanism of action of antitumor drugs from the molecular point of view and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents, aiming at the rationalization of the action of this type of drug, which would allow the design of new active structures. * Explains the biological basis of cancer treatment and the role of chemists in improving anticancer drugs * Provides the historical background and serves as a comprehensive and practical guide on cancer research and anticancer drug development * Includes coverage of different approaches to treating cancer, drug resistance, and a chapter on cancer prevention

Medicinal Chemistry

A Molecular and Biochemical Approach

Author: Thomas Nogrady

Publisher: Oxford University Press

ISBN:

Category: Medical

Page: 649

View: 522

Fully updated, this textbook takes a receptor-based, target-centred approach, presenting concepts central to the study of drug action in a logical, mechanistic way, grounded on molecular & biochemical principles.

Enzyme Kinetics: Catalysis and Control

A Reference of Theory and Best-Practice Methods

Author: Daniel L. Purich

Publisher: Elsevier

ISBN:

Category: Science

Page: 920

View: 605

Far more than a comprehensive treatise on initial-rate and fast-reaction kinetics, this one-of-a-kind desk reference places enzyme science in the fuller context of the organic, inorganic, and physical chemical processes occurring within enzyme active sites. Drawing on 2600 references, Enzyme Kinetics: Catalysis & Control develops all the kinetic tools needed to define enzyme catalysis, spanning the entire spectrum (from the basics of chemical kinetics and practical advice on rate measurement, to the very latest work on single-molecule kinetics and mechanoenzyme force generation), while also focusing on the persuasive power of kinetic isotope effects, the design of high-potency drugs, and the behavior of regulatory enzymes. Historical analysis of kinetic principles including advanced enzyme science Provides both theoretical and practical measurements tools Coverage of single molecular kinetics Examination of force generation mechanisms Discussion of organic and inorganic enzyme reactions

Introduction to Pharmacology, Third Edition

Author: Mannfred A. Hollinger

Publisher: CRC Press

ISBN:

Category: Medical

Page: 432

View: 565

The first edition of Introduction to Pharmacology has over recent years become a highly influential text among students wishing to acquire a knowledge of pharmacology without having to refer to the larger, more detailed, traditional pharmacology volumes. This revised and updated second edition contains significant new material to bring the reader up-to-date with the latest practices and principles in pharmacology. Exploring the basic principles in both the therapeutic and toxicological aspects of drug use, the book employs contemporary examples of medication, supplemented with an increased number of accurate and easy-to-interpret figures and diagrams. Additionally, Introduction to Pharmacology presents the important concept of understanding the limitations surrounding the drugs that cure, replace physiological inadequacies, or treat symptoms, and which have led to the system of drug classification. The broad scope of the book also encompasses the role of the FDA, drugs in sport, and the use of animals for drug experimentation. A clear and accessible book, Introduction to Pharmacology builds on the strengths of the first edition and is an invaluable reference for all students interested in this subject.

Sigma- Aldrich Labware

Author:

Publisher:

ISBN:

Category:

Page:

View: 321

Evaluation of Enzyme Inhibitors in Drug Discovery

A Guide for Medicinal Chemists and Pharmacologists

Author: Robert A. Copeland

Publisher: Wiley-Interscience

ISBN:

Category: Medical

Page: 271

View: 644

Vital information for discovering and optimizing new drugs "Understanding the data and the experimental details that support it has always been at the heart of good science and the assumption challenging process that leads from good science to drug discovery. This book helps medicinal chemists and pharmacologists to do exactly that in the realm of enzyme inhibitors." —Paul S. Anderson, PhD This publication provides readers with a thorough understanding of enzyme-inhibitor evaluation to assist them in their efforts to discover and optimize novel drug therapies. Key topics such as competitive, noncompetitive, and uncompetitive inhibition, slow binding, tight binding, and the use of Hill coefficients to study reaction stoichiometry are all presented. Examples of key concepts are presented with an emphasis on clinical relevance and practical applications. Targeted to medicinal chemists and pharmacologists, Evaluation of Enzyme Inhibitors in Drug Discovery focuses on the questions that they need to address: What opportunities for inhibitor interactions with enzyme targets arise from consideration of the catalytic reaction mechanism? How are inhibitors evaluated for potency, selectivity, and mode of action? What are the advantages and disadvantages of specific inhibition modalities with respect to efficacy in vivo? What information do medicinal chemists and pharmacologists need from their biochemistry and enzymology colleagues to effectively pursue lead optimization? Beginning with a discussion of the advantages of enzymes as targets for drug discovery, the publication then explores the reaction mechanisms of enzyme catalysis and the types of interactions that can occur between enzymes and inhibitory molecules that lend themselves to therapeutic use. Next are discussions of mechanistic issues that must be considered when designing enzyme assays for compound library screening and for lead optimization efforts. Finally, the publication delves into special forms of inhibition that are commonly encountered in drug discovery efforts, but can be easily overlooked or misinterpreted. This publication is designed to provide students with a solid foundation in enzymology and its role in drug discovery. Medicinal chemists and pharmacologists can refer to individual chapters as specific issues arise during the course of their ongoing drug discovery efforts.

Remington

The Science and Practice of Pharmacy

Author: Joseph Price Remington

Publisher: Lippincott Raven

ISBN:

Category: Drugs

Page: 2077

View: 503

For more than 100 years, this textbook has been the definitive reference for all aspects of the science and practice of pharmacy, and is used for pharmaceutics, therapeutics and pharmacy practice courses in primary curricula. Since the first edition was published, pharmacists have used this book as a key one-stop reference. This updated edition covers many education and practice issues, from the history of pharmacy and ethics, to industrial pharmacy and pharmacy practice. New to the edition are expanded sections on pharmacy administration and patient care, which include new topics such as: nutrition in pharmacy practice; self care and home diagnostic products; health care delivery systems and interdisciplinary care; and home health patient care. Also, information has been condensed into one volume for greater portability and convenience.

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