Drug Stereochemistry


Book Description

Maintaining and enhancing its focus on key issues in the development, regulatory approval and use of stereoisomeric compounds, this edition continues to cover in detail all aspects of chiral drugs from the academic, governmental, industrial and clinical points of view.;Completely rewritten and updated throughout, Drug Stereochemistry: illustrates current indirect chromatographic methods for the resolution of drug enantiomers; treats the rapidly growing area of enantioselective gas chromatography; discusses the latest in HPLC resolution of enantiomeric drugs; uses verapamil as a model to show how stereoselective pharmacokinetics affect pharmacodynamics; and supplies an in-depth study on the effect of stereoselective plasma protein binding.;This edition offers entirely new chapters that: discuss the recent decisions and present position of the US Food and Drug Administration on the development of stereoisomeric drugs; explicate enzymatic synthesis of stereochemically pure drugs; review the toxicological, pharmacokinetic and pharmacodynamic differences found among stereoisomers; elucidate the stereoselective transport of drugs across epithelia; and give a physician's perspective on the questions and problems caused by stereoisomeric drugs in practice as well as the pharmaceutical industry's collective viewpoint based on a national survey.




Drug Stereochemistry


Book Description

Drug Stereochemistry: Analytical Methods and Pharmacology, Third Edition covers all aspects of chiral drugs from academic, governmental, industrial, and clinical perspectives, reflecting the many advances in techniques and methodology. Topics include:The use of enzymes in the synthesis and resolution of enantiometrically pure compounds in drug disc




Stereochemical Aspects of Drug Action and Disposition


Book Description

This book aims to guide and inspire drug researchers as they enter the 21st century. Stereochemistry is an essential dimension in pharmacology and should be understood as such by all drug researchers whatever their background. When used as probes or medicines, stereoisomeric drugs offer invaluable insights or innovative therapeutic strategies. The book spans the subject from the molecular to the clinical. The first section on chemical aspects contains chapters on chemical synthesis, analysis, natural products, chiral stability (racemezation) and physical properties. The second section is on experimental pharmacology, with chapters on drug-receptor interactions, chiral recognition, ion channels, and molecular toxicology. The third section focuses on drug disposition, with chapters on absorption, distribution, protein binding, metabolism and elimination. The final section is dedicated to regulatory and clinical aspects.




The Organic Chemistry of Drug Design and Drug Action


Book Description

Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. - New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations - Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years - Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization




Introduction to Stereochemistry


Book Description

CHEMISTRY STUDENT GUIDES. GUIDED BY STUDENTS Why did the drug thalidomide cause birth defects? What is the chemical difference between sucrose and lactose in your food? Stereochemistry holds the answer and is essential to the understanding of the chemistry of life. Stereochemistry is an important concept that often causes confusion amongst students when they learn it for the first time. Unlike most other areas of chemistry, it requires the chemist to visualise molecules in 3D, which can be difficult. In this book we deal with tricky concepts like conformation and configuration, how to represent them accurately and how to use the correct terms to describe them in both organic and inorganic chemistry. We involved students in the writing process to ensure we deal with areas that you find difficult, in an understandable language. With problems designed to focus on common errors and misconceptions, real life examples, and practical hands-on exercises coupled with visualisation tips, our intention is to give you the tools to become confident in stererochemistry. Complementing mainstream organic textbooks, or self-study, this book is for anyone who has struggled with describing alkenes as E or Z, assigning R and S absolute configurations, drawing Newman projections or chair representations of cyclohexanes, axial chirality, understanding the stereochemistry of octahedral metal complexes and indeed explaining complexities observed in NMR spectra. Chemistry Student Guides are written with current students involved at every stage, guiding the books towards the most challenging aspects of the topic. Student co-authors for Introduction to Stereochemistry are Caroline Akamune, Michael Lloyd and Matthew Taylor.




Chirality in Drug Design and Development


Book Description

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.




The Organic Chemistry of Medicinal Agents


Book Description

The most concise and streamlined textbook available on organic chemistry for the pharmacy student Organic Chemistry for Pharmacy is a textbook written specifically for the students taking the required Organic/Medical Pharmacy course. Using a building-block approach, the book delivers a basic, yet thorough discussion of the mode of action, therapeutic applications, and limitations of various pharmaceutical agents. Organic Chemistry for Pharmacy is especially written for students who have a limited background in chemistry. In order to make the learning/teaching experience as efficient as possible, Organic Chemistry for Pharmacy includes outstanding pedagogical features such as chapter outlines, chapter summaries, boxed “take away points”, quick-reference tables, and problems within each chapter. The focus and presentation of this text is particularly suited for Organic/Medical Pharmacy courses which are weighted heavily towards Organic, rather than Medical Pharmacy.




Chirality in Drug Research


Book Description

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.




Strategies for Organic Drug Synthesis and Design


Book Description

This book examines and evaluates the strategies utilized to design and synthesize pharmaceutically active agents. Significant updates over the last 10 years since the publication of the 1st edition include synthesis of enantiomerically pure isomers, novel chemical methodologies, and new pharmaceutical agents targeted at novel biological endpoints. Written by an experienced successful author, this book meets the needs of a growing community of researchers in pharmaceutical R &D, as well as medical professionals, by providing a useful guide for designing and synthesizing pharmaceutical agents. Additionally, it is a useful text for medicinal chemistry students.




Basic Concepts in Medicinal Chemistry


Book Description

Medicinal chemistry is a complex topic. Written in an easy to follow and conversational style, Basic Concepts in Medicinal Chemistry focuses on the fundamental concepts that govern the discipline of medicinal chemistry as well as how and why these concepts are essential to therapeutic decisions. The book emphasizes functional group analysis and the basics of drug structure evaluation. In a systematic fashion, learn how to identify and evaluate the functional groups that comprise the structure of a drug molecule and their influences on solubility, absorption, acid/base character, binding interactions, and stereochemical orientation. Relevant Phase I and Phase II metabolic transformations are also discussed for each functional group. Key features include: • Discussions on the roles and characteristics of organic functional groups, including the identification of acidic and basic functional groups. • How to solve problems involving pH, pKa, and ionization; salts and solubility; drug binding interactions; stereochemistry; and drug metabolism. • Numerous examples and expanded discussions for complex concepts. • Therapeutic examples that link the importance of medicinal chemistry to pharmacy and healthcare practice. • An overview of structure activity relationships (SARs) and concepts that govern drug design. • Review questions and practice problems at the end of each chapter that allow readers to test their understanding, with the answers provided in an appendix. Whether you are just starting your education toward a career in a healthcare field or need to brush up on your organic chemistry concepts, this book is here to help you navigate medicinal chemistry. About the Authors Marc W. Harrold, BS, Pharm, PhD, is Professor of Medicinal Chemistry at the Mylan School of Pharmacy, Duquesne University, Pittsburgh, PA. Professor Harrold is the 2011 winner of the Omicron Delta Kappa "Teacher of the Year" award at Duquesne University. He is also the two-time winner of the "TOPS" (Teacher of the Pharmacy School) award at the Mylan School of Pharmacy. Robin M. Zavod, PhD, is Associate Professor for Pharmaceutical Sciences at the Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, where she was awarded the 2012 Outstanding Faculty of the Year award. Professor Zavod also serves on the adjunct faculty for Elmhurst College and the Illinois Institute of Technology. She currently serves as Editor-in-Chief of the journal Currents in Pharmacy Teaching and Learning.