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Chirality in Drug Design and Development

Chirality in Drug Design and Development Author Indra K. Reddy
ISBN-10 9780824751098
Release 2004-03-15
Pages 1200
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Covering every essential element in the development of chiral products, this reference provides a solid overview of the formulation, biopharmaceutical characteristics, and regulatory issues impacting the production of these pharmaceuticals. It supports researchers as they evaluate the pharmacodynamic, pharmacokinetic, and toxicological characteristics of specific enantiomers and chiral drug compounds and addresses in one convenient reference all the major challenges pertaining to drug chirality that have been neglected in the literature. Chirality in Drug Design and Development collects the latest studies from an interdisciplinary team of experts on chiral drug design.



Chirality in Drug Design and Synthesis

Chirality in Drug Design and Synthesis Author C. Brown
ISBN-10 9781483288246
Release 2013-10-22
Pages 243
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Chirality in Drug Design and Synthesis is a collection of papers that discusses the property of asymmetry in the structural and synthetic chemistry of natural products, including the significance of chirality in medicinal chemistry. These papers examine the need for the preparation and study of pure enantiomers of chiral drug substances and their mechanism of interaction with enzymes and receptors. These papers also investigate the techniques in studying these interactions, as well as analyze the methods for their synthesis in enantiomerically pure form. One paper discusses the pharmacological and pharmacokinetic analyses made that point to the differences in the activity and disposition of enantiometric pairs. Another paper reviews the implications of the neglect of stereoselectivity at the different levels during the examination process of racemic drugs. Since no general guidelines exists for the development of drugs with chiral centers, one paper suggests a case-by-case approach in evaluating the safety and efficacy of drugs, particularly as regards how isomers differ in their effects. This collection is suitable for the pharmacologist, medicinal chemists, toxicologists, mechanistic chemists and synthetic organic chemists.



Chirality in Drug Research

Chirality in Drug Research Author Eric Francotte
ISBN-10 9783527608713
Release 2007-09-24
Pages 368
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Divided into the three main sections of synthesis, analysis and drug development, this handbook covers all stages of the drug development process, including large-scale synthesis and purification of chirally pure pharmaceuticals. The two editors from academia and a major pharmaceutical company have assembled an experienced, international team who provide first-hand practical advice and report previously unpublished data. In the first section, the isolation of chiral drugs from natural sources, their production in enzymatic processes and the resolution of racemic mixtures in preparative chromatography are outlined in separate chapters. For the section on qualitative and quantitative analysis, enantioselective chromatographic methods are presented as well as optical methods and CE-MS, while the final section deals with the pharmacology, pharmacokinetics and metabolic aspects of chiral drugs, devoting whole chapters to stereoselective drug binding and modeling chiral drug-receptor interactions. With its unique industry-relevant aspects, this is a must for medicinal and pharmaceutical chemists.



The Impact of Stereochemistry on Drug Development and Use

The Impact of Stereochemistry on Drug Development and Use Author Hassan Y. Aboul-Enein
ISBN-10 CHI:44554172
Release 1997-04-11
Pages 728
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Provides an authoritative source of practical information on stereochemistry and its impact on drug development. Unlike other books which focus on synthesis, this work explores analytical, pharmacological, and regulatory topics in dealing with the theory and practice of stereochemistry in the pharmaceutical industry today. It specifically addresses how the body metabolizes chiral molecules; the varying effects of different chiral molecules; and provides detailed evaluations of current seperation techniques. Includes regulatory information.



The Organic Chemistry of Drug Design and Drug Action

The Organic Chemistry of Drug Design and Drug Action Author Richard B. Silverman
ISBN-10 9780123820310
Release 2014-03-29
Pages 536
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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



Basic Principles of Drug Discovery and Development

Basic Principles of Drug Discovery and Development Author Benjamin Blass
ISBN-10 9780124115255
Release 2015-04-24
Pages 580
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Basic Principles of Drug Discovery and Development presents the multifaceted process of identifying a new drug in the modern era, providing comprehensive explanations of enabling technologies such as high throughput screening, structure based drug design, molecular modeling, pharmaceutical profiling, and translational medicine, all areas that have become critical steps in the successful development of marketable therapeutics. The text introduces the fundamental principles of drug discovery and development, also discussing important drug targets by class, in vitro screening methods, medicinal chemistry strategies in drug design, principles in pharmacokinetics and pharmacodynamics, animal models of disease states, clinical trial basics, and selected business aspects of the drug discovery process. It is designed to enable new scientists to rapidly understand the key fundamentals of drug discovery, including pharmacokinetics, toxicology, and intellectual property." Provides a clear explanation of how the pharmaceutical industry works Explains the complete drug discovery process, from obtaining a lead, to testing the bioactivity, to producing the drug, and protecting the intellectual propertyIdeal for anyone interested in learning about the drug discovery process and those contemplating careers in the industry Explains the transition process from academia or other industries



The Practice of Medicinal Chemistry

The Practice of Medicinal Chemistry Author Camille Georges Wermuth
ISBN-10 9780124172135
Release 2015-07-01
Pages 902
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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



New Developments in Medicinal Chemistry

New Developments in Medicinal Chemistry Author Carlton Anthony Taft
ISBN-10 9781608059546
Release 2014-10-10
Pages 250
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This e-book series is recommended for readers who are interested in or work with current theoretical and experimental research in medicinal chemistry, with an emphasis on computer aided-drug design and organic synthesis for therapeutic purposes. The e-book series encompasses the multidisciplinary field of medicinal chemistry which overlaps the knowledge of chemistry, physics, biochemistry, biology and pharmacology. The second volume of the series contains the following topics: -Current State-of-the-Art for Virtual Screening and Docking Methods -Estimating Protein-Ligand Binding Affinity by NMR -ADME/Tox Predictions in Drug Design -Bioisosteric Replacements in Drug Design



Chiral Drugs

Chiral Drugs Author Guo-Qiang Lin
ISBN-10 1118075633
Release 2011-08-08
Pages 528
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An integrated view of chiral drugs—from concept and synthesisto pharmaceutical properties Chirality greatly influences a drug's biological and pharmacological properties. In an effort to achieve more predictable results from chiral drugs, the Food and Drug Administration now requires that these medicines be as pure as possible, which places great demands on drug synthesis, purification, analysis, and testing. To assist researchers in acquiring the essential knowledge to meet these rigid guidelines, Chiral Drugs focuses on three vital chiral technologies—asymmetric synthesis, biocatalytic process, and chiral resolution—to offer details on the basic concepts, key developments, and recent trends in chiral drug discovery, along with: The history of chiral drugs development and industrial applications of chiral technologies A section listing twenty-five approved or advanced-trial chiral drugs that lists each drug name, chemical name and properties, a representative synthetic pathway, pharmacological characterizations, and references An interdisciplinary approach combining synthetic organic chemistry, medicinal chemistry, and pharmacology Nearly two-thirds of the drugs on today's market are chiral drugs. Reducing and eliminating their negative characteristics is an ongoing and serious challenge for the pharmaceutical industry. With its well-balanced approach to covering each important aspect of chirality, Chiral Drugs champions important strategies for tipping the medical scale in a positive direction for the production of more effective—and safer—drugs.



Drug Like Properties

Drug Like Properties Author Li Di
ISBN-10 9780128013229
Release 2015-12-17
Pages 580
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Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, only a fraction have sufficient ADME (absorption, distribution, metabolism, elimination) properties, and acceptable toxicology properties, to become a drug product that will successfully complete human Phase I clinical trials. Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization, Second Edition, provides scientists and students the background and tools to understand, discover, and develop optimal clinical candidates. This valuable resource explores physiochemical properties, including solubility and permeability, before exploring how compounds are absorbed, distributed, and metabolized safely and stably. Review chapters provide context and underscore the importance of key concepts such as pharmacokinetics, toxicity, the blood-brain barrier, diagnosing drug limitations, prodrugs, and formulation. Building on those foundations, this thoroughly updated revision covers a wide variety of current methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties for process and product improvement. From conducting key assays for interpretation and structural analysis, the reader learns to implement modification methods and improve each ADME property. Through valuable case studies, structure-property relationship descriptions, and structure modification strategies, Drug-Like Properties, Second Edition, offers tools and methods for ADME/Tox scientists through all aspects of drug research, discovery, design, development, and optimization. Provides a comprehensive and valuable working handbook for scientists and students in medicinal chemistry Includes expanded coverage of pharmacokinetics fundamentals and effects Contains updates throughout, including the authors’ recent work in the importance of solubility in drug development; new and currently used property methods, with a reduction of seldom-used methods; and exploration of computational modeling methods



Metabolite Safety in Drug Development

Metabolite Safety in Drug Development Author Suzanne L. Iverson
ISBN-10 9781118949658
Release 2016-08-01
Pages 352
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A reference on drug metabolism and metabolite safety in the development phase, this book reviews the analytical techniques and experimental designs critical for metabolite studies. It features case studies of lessons learned and real world examples, along with regulatory perspectives from the US FDA and EMA. • Reviews the analytical techniques and experimental designs critical for metabolite studies • Covers methods including chirality, species differences, mass spectrometry, radiolabels, and in vitro / in vivo correlation • Discusses target pharmacology, in vitro systems aligned to toxicity tests, and drug-drug interactions • Includes perspectives from authors with firsthand involvement in industry and the study of drug metabolites, including viewpoints that have influenced regulatory guidelines



Smith and Williams Introduction to the Principles of Drug Design and Action Fourth Edition

Smith and Williams  Introduction to the Principles of Drug Design and Action  Fourth Edition Author H. John Smith
ISBN-10 0203304152
Release 2005-10-10
Pages 720
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Advances in knowledge and technology have revolutionized the process of drug development, making it possible to design drugs for a given target or disease. Building on the foundation laid by the previous three editions, Smith and Williams’ Introduction to the Principles of Drug Design and Action, Fourth Edition includes the latest information on topics such as gene therapy, computer-aided design, and molecular techniques including proteomics. Using real-world examples that illustrate the principles of drug design, the author explores the discovery of lead compounds and their manipulation in the production of non-toxic, metabolically stable drug candidates that will interact with target receptors in a predicted fashion. See what’s new in the Fourth Edition: Fully updates and expands the contents Coverage of agonists and antagonists of neuro-transmitters Information on the design of stable peptide-like drugs The human genome and its impact on drug discovery and development Advances in therapy and pharmacokinetics Adopting a from-the-bench-to-the-marketplace approach, the book provides a thorough grounding in rational drug design. It emphasizes principles and elucidates a framework for basic drug design into which current and, more importantly, future drugs will fit.



Photostability of Drugs and Drug Formulations Second Edition

Photostability of Drugs and Drug Formulations  Second Edition Author Hanne Hjorth Tonnesen
ISBN-10 1420023594
Release 2004-06-29
Pages 448
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Providing the guidance needed for formulation, handling, and quality control of photolabile drugs, Photostability of Drugs and Drug Formulations, Second Edition explores the significance of new information on drug photoreactivity in a pharmaceutical context. Completely revised and updated, with chapter authors drawn from an international panel of experts, the book supplies the background necessary for planning standardized photochemical stability studies as a part of drug development and formulation work. It contains comprehensive coverage of the physical and chemical aspects of drug photoreactivity, formulation, stability testing, and drug design/discovery in one resource. The contents have been reorganized to focus on the standardization of photostability testing of drug substances and products, in vitro photoreactivity screening of drugs, and various aspects of the formulation of photoreactive substances. The information on in vitro screening of drug photoreactivity is of great relevance for scientists who are developing and validating a set of testing protocols to address photosafety. Discussing kinetic and chemical aspects of drug photodecomposition as well as the practical problems frequently encountered in photochemical stability testing, this book helps you design a test protocol and interpret the results. Features Assists non-experts in this field design a test protocol and interpret the results Covers in vitro and in vivo aspects of interactions between drugs and light Explores the kinetic and chemical aspects of drug photodecomposition Discusses the problems frequently encountered in photochemical stability testing Provides guidance on how to address photosafety assessments and labeling requirements of potentially photoreactive drugs Highlights the practical implications of drug photodecomposition from a pharmaceutical viewpoint Offers specific guidance in photostability testing and screening of drug photoreactivity



Bioorganometallic Chemistry

Bioorganometallic Chemistry Author Gérard Jaouen
ISBN-10 9783527335275
Release 2015-04-20
Pages 398
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An up-to-date reference reflecting the significant advances and important breakthroughs made in this emerging discipline over the last decade. As such, the book provides an overview of the latest developments and future trends in the field, focusing on such applications as the development of potentially active organometallic drugs against incurable diseases, as well as in such areas as catalysis, energy, analytical chemistry, and imaging. The renowned editor, who established the term "bioorganometallics", and his international team of experts have put together a valuable resource for researchers in organometallic, inorganic, medicinal, and biochemistry.



Smith and Williams Introduction to the Principles of Drug Design and Action Fourth Edition

Smith and Williams  Introduction to the Principles of Drug Design and Action  Fourth Edition Author H. John Smith
ISBN-10 0203304152
Release 2005-10-10
Pages 720
Download Link Click Here

Advances in knowledge and technology have revolutionized the process of drug development, making it possible to design drugs for a given target or disease. Building on the foundation laid by the previous three editions, Smith and Williams’ Introduction to the Principles of Drug Design and Action, Fourth Edition includes the latest information on topics such as gene therapy, computer-aided design, and molecular techniques including proteomics. Using real-world examples that illustrate the principles of drug design, the author explores the discovery of lead compounds and their manipulation in the production of non-toxic, metabolically stable drug candidates that will interact with target receptors in a predicted fashion. See what’s new in the Fourth Edition: Fully updates and expands the contents Coverage of agonists and antagonists of neuro-transmitters Information on the design of stable peptide-like drugs The human genome and its impact on drug discovery and development Advances in therapy and pharmacokinetics Adopting a from-the-bench-to-the-marketplace approach, the book provides a thorough grounding in rational drug design. It emphasizes principles and elucidates a framework for basic drug design into which current and, more importantly, future drugs will fit.



Mirror Image Asymmetry

Mirror Image Asymmetry Author James P. Riehl
ISBN-10 047058887X
Release 2011-04-22
Pages 184
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An overview of the importance and consequences of asymmetry from molecules to the macroscopic world As scientists have become more capable of probing the structure of three-dimensional objects at the molecular level, the need to understand the concept and the consequences of mirror-image asymmetry—chirality—has increased enormously. Written at an introductory level, Mirror-Image Asymmetry provides an overview of the importance and effects of asymmetry from the atomic and molecular world of physics and chemistry to the organisms and structures that we see and use in our everyday life. The reader will develop a broad appreciation of three-dimensional asymmetry from the microscopic molecular world to the macroscopic world of handedness, automobile driving, windmills, sports, and similar phenomena. The book features: An introduction to basic definitions and the nomenclature of asymmetric and dissymmetric molecules Up-to-date examples of the importance and consequences of asymmetry in modern drug applications, current theories of the origin of asymmetry in nature, and examples of molecular asymmetry in smell, taste, and insect communication Many illustrations, chemical structures, and photographs that enable the reader to connect the actual asymmetrical structures to the different phenomena that depend on structural asymmetry In the 150 years since Louis Pasteur discovered asymmetry in molecular structures, scientists have made great progress in understanding how interactions between chiral molecules influence biochemical processes. This knowledge is leading to very sophisticated asymmetric synthetic techniques that have greatly benefitted many research groups especially those in the pharmaceutical industry. This guide to the role of molecular and macroscopic chirality will inspire students and scientists in chemistry, biology, physics, and drug discovery.



Medicinal Chemistry

Medicinal Chemistry Author Thomas Nogrady
ISBN-10 9780190282967
Release 2005-08-11
Pages
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Fully updated and rewritten by a basic scientist who is also a practicing physician, the third edition of this popular textbook remains comprehensive, authoritative and readable. Taking a receptor-based, target-centered approach, it presents the concepts central to the study of drug action in a logical, mechanistic way grounded on molecular and principles. Students of pharmacy, chemistry and pharmacology, as well as researchers interested in a better understanding of drug design, will find this book an invaluable resource. Starting with an overview of basic principles, Medicinal Chemistry examines the properties of drug molecules, the characteristics of drug receptors, and the nature of drug-receptor interactions. Then it systematically examines the various families of receptors involved in human disease and drug design. The first three classes of receptors are related to endogenous molecules: neurotransmitters, hormones and immunomodulators. Next, receptors associated with cellular organelles (mitochondria, cell nucleus), endogenous macromolecules (membrane proteins, cytoplasmic enzymes) and pathogens (viruses, bacteria) are examined. Through this evaluation of receptors, all the main types of human disease and all major categories of drugs are considered. There have been many changes in the third edition, including a new chapter on the immune system. Because of their increasingly prominent role in drug discovery, molecular modeling techniques, high throughput screening, neuropharmacology and genetics/genomics are given much more attention. The chapter on hormonal therapies has been thoroughly updated and re-organized. Emerging enzyme targets in drug design (e.g. kinases, caspases) are discussed, and recent information on voltage-gated and ligand-gated ion channels has been incorporated. The sections on antihypertensive, antiviral, antibacterial, anti-inflammatory, antiarrhythmic, and anticancer drugs, as well as treatments for hyperlipidemia and peptic ulcer, have been substantially expanded. One new feature will enhance the book's appeal to all readers: clinical-molecular interface sections that facilitate understanding of the treatment of human disease at a molecular level.