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.

"This updated and expanded edition of the popular textbook, Basic Concepts in Medicinal Chemistry, has been enhanced with new subject material, numerous self-assessment tools and special features to advance and strengthen the learning process. Designed to help students incrementally build their knowledge of fundamental concepts of medicinal chemistry and their applications to therapeutic decisions, it is progressively organized. The text is also enhanced to make potentially confusing concepts easier to understand. Numerous examples and review questions further reinforce learning and analytical skills"--Publisher's description.

Functional group characteristics and roles -- Identifying acidic and basic functional groups -- Solving pH and pKa problems -- Salts and solubility -- Drug binding interactions -- Stereochemistry and drug action -- Drug metabolism -- Structure activity relationships and basic concepts in drug design

Organic Chemistry Concepts and Applications for Medicinal Chemistry provides a valuable refresher for understanding the relationship between chemical bonding and those molecular properties that help to determine medicinal activity. This book explores the basic aspects of structural organic chemistry without going into the various classes of reactions. Two medicinal chemistry concepts are also introduced: partition coefficients and the nomenclature of cyclic and polycyclic ring systems that comprise a large number of drug molecules. Given the systematic name of a drug, the reader is guided through the process of drawing an accurate chemical structure. By emphasizing the relationship between structure and properties, this book gives readers the connections to more fully comprehend, retain, apply, and build upon their organic chemistry background in further chemistry study, practice, and exams. - Focused approach to review those organic chemistry concepts that are most important for medicinal chemistry practice and understanding - Accessible content to refresh the reader's knowledge of bonding, structure, functional groups, stereochemistry, and more - Appropriate level of coverage for students in organic chemistry, medicinal chemistry, and related areas; individuals seeking content review for graduate and medical courses and exams; pharmaceutical patent attorneys; and chemists and scientists requiring a review of pertinent material

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

A slow and consistent study of the approaches for drug design can help the foundation for a good scientific intuition. This edition includes over 30 new illustrations, numerous new mechanistic schemes and enhanced original figures. In addition, the use of color makes its study more pleasant and impressive. The Second Edition has been thoroughly revised with a modern look. The chapters on QSAR and Drug Metabolism have been extended, emphasizing concepts, such as the hyperconjugative effect or the anomeric effect, in which the student normally finds it difficult to understand. Stereoelectronic effects are essential to explain the mechanism of action of drugs and therefore, its agile and intuitive handling will allow the student access to both chemical and biological mechanisms, in a more rational way. The text is illustrated with hundreds of formulas and many tables that facilitate the understanding of this interesting discipline, which is halfway between Organic Chemistry, Biochemistry and Pharmacology. This Volume is aimed at building basis principles on drug design and it is likely to be of interest to students reading, pharmacy, pharmacology, and pharmaceutical chemistry. This book emphasizes general principles of drug design and drug action from an organic chemical perspective, rather than from the overview of specific classes of drugs, allowing the reader to extrapolate information to many related classes of drug molecules. This volume presents an organic chemistry’s perspective of how drug are designed and assuming no prior knowledge of biochemistry, and pharmacology. It is written in an informal, clear style so that undergraduates can easily understand the concepts presented.

Medicinal Chemistry begins with the history of the field, starting from the serendipitous use of plant preparations to current practice of design- and target-based screening methods. Written from the perspective of practicing medicinal chemists, the text covers key drug discovery activities such as pharmacokinetics and patenting, as well as the classes and structures of drug targets (receptors, enzymes, nucleic acids, and protein-protein and lipid interactions) with numerous examples of drugs acting at each type. Selected therapeutic areas include drugs to treat cancer, infectious diseases, and central nervous system disorders. Throughout the book, historical and current examples illustrate the progress to market and case studies explore the applications of concepts discussed in the text. Each chapter features a Journal Club, as well as review and application questions to enhance and test comprehension. This textbook is ideal for upper-level undergraduates and graduate students taking a one-semester survey course on medicinal chemistry and/or drug discovery, as well as scientists entering the pharmaceutical industry.

Medicinal Chemistry: Fundaments presents the cycle of the life of drugs, their physico-chemical properties, and consequences that arise in development. The fundamental concepts of Medicinal Chemistry (pharmacophore, prodrugs, Lipinsky rules) are also presented, including discussions on specific concerns of the European Pharmacopeia – the industrialist's bible – its role, and a description of the monographs of active principles. - Defines the lifecycle of drugs - Explains the physico-chemical properties and consequences of a drug - Studies the fundamental concepts of medicinal chemistry - Describes the active ingredient monographs

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.

Introduction to Drug Synthesis explores the central role played by organic synthesis in the process of drug design and development - from the generation of novel drug structures to the improved efficiency of large scale synthesis.