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"Advanced Medicinal Chemistry - A Practical Guide" to suit the requirements of postgraduate (PG) students of pharmaceutical chemistry, pharmaceutical analysis, quality assurance, pharmacognosy, phytochemistry. It is useful to PG students of chemistry, biotechnology and allied fields too.
Emphasizing applications of chemistry while reinforcing theory – especially in the areas of organic and physical chemistry – this new text prepares readers for career success in the pharmaceutical, medical, and biotech industries. Medicinal Chemistry: The Modern Drug Discovery Process delivers a comprehensive introduction to medicinal chemistry at an appropriate level of detail for a diverse range of readers. By highlighting the concepts and skills related to drug discovery, Stevens deepens readers' understanding of the knowledge and techniques necessary for their careers.
Drug discovery is a constantly developing and expanding area of research. Developed to provide a comprehensive guide, the Handbook of Medicinal Chemistry covers the past, present and future of the entire drug development process. Highlighting the recent successes and failures in drug discovery, the book helps readers to understand the factors governing modern drug discovery from the initial concept through to a marketed medicine. With chapters covering a wide range of topics from drug discovery processes and optimization, development of synthetic routes, pharmaceutical properties and computational biology, the handbook aims to enable medicinal chemists to apply their academic understanding to every aspect of drug discovery. Each chapter includes expert advice to not only provide a rigorous understanding of the principles being discussed, but to provide useful hints and tips gained from within the pharmaceutical industry. This expertise, combined with project case studies, highlighting and discussing all areas of successful projects, make this an essential handbook for all those involved in pharmaceutical development.
Advances in Medicinal Chemistry Research is a book addressed to undergraduate and postgraduate students, where recent advances in the discovery and development of effective agents against the most remarkable wide-reaching diseases are presented, divided into seven chapters. This first edition of Advances in Medicinal Chemistry Research offers insights into medicinal chemistry that arguably have the most significant impact on our lives than any other. It draws together research on therapeutic agents from natural, synthetic, and virtual screening sources as starting points for the design of drugs against obesity, multidrug-resistant bacteria, neglected tropical diseases, Alzheimer, and cancer. From the prediction of promising hits and identification of active compounds to the extraction of more complex molecules, this book explores a range of essential topics to support the development of novel, economical, and efficacious therapeutics for these diseases, which currently affect a billion people worldwide. Beginning with an overview of obesity, showing the current research landscape, the books shows the importance of natural and synthetic products as promising anti-obesity agents. Subsequently, the medicinal chemistry of modulation of bacterial resistance is presented, focusing on the MFS, RND, ABC, and MATE superfamilies. The book goes on to discuss such topics as antituberculosis, antileishmanial, and anti-hepatitis thiophene-containing compounds, under the medicinal chemistry point of view. Also, potent human glutaminyl cyclase inhibitors are deeply discussed and displayed as hopeful anti-Alzheimer's agents. The last three chapters are focused on the development of researches involving new anticancer agents, initializing with LBDD, SBDD, QSAR, and QM/MM methods applied to the identification of novel promising anticancer compounds. Moreover, IDO1 inhibitors are exhaustively explored and analyzed as a new promise for the immunotherapy of cancer. Finally, a great update on Eg5 kinesin inhibitors is provided, exploring different chemical classes of synthetic and natural compounds, including miscellanea as a new approach for Eg5 inhibition. Combining the expertise of researchers from around the world, this volume aims to support and encourage researches for the development of novel, safe, and active agents against lipase enzyme, bacteria, neglected tropical diseases, Alzheimer, and cancer. The clear narrative truly engages the reader, holding their attention right from the opening of a chapter, and maintaining interest and understanding as a chapter leads into more complex material. Advances in Medicinal Chemistry Research is a book that reviews ongoing developments and recent cutting-edge advances in medicinal chemistry of the most relevant diseases found nowadays, underlining how medicinal chemistry research continues to make significant contributions to the discovery and development of new therapeutic entities. Key Features â¢Chapters written by active specialists and leading experts deeply engaged in the research field of most deadly and limiting diseases for drug discovery. â¢Draws together cutting-edge research advances in medicinal chemistry focused at the obesity, multidrug-resistant microorganisms, Alzheimer, and cancer in a single volume. â¢Highlights the future potential of researches for the medicinal chemistry of most impactful diseases today. â¢Contents addressed to medicinal chemistry, biochemistry, biology, and pharmacy students, professors, and researchers.
Provides a thorough overview of the role of fluorine in pharmaceutical science and development Includes chapters on fluorinated analogues of natural products, fluorinated amino acids and peptides, and derivatives of sugars Classifies marketed and in-development fluorinated pharmaceuticals according to their therapeutic classes
Accounts in Drug Discovery describes recent case studies in medicinal chemistry with a particular emphasis on how the inevitable problems that arise during any project can be surmounted or overcome. The Editors cover a wide range of therapeutic areas and medicinal chemistry strategies, including lead optimization starting from high-throughput screening "hits" as well as rational, structure-based design. The chapters include "follow-ons" and "next generation" compounds that aim to improve upon first-generation agents. This volume surveys the range of challenges commonly faced by medicinal chemistry researchers, including the optimization of metabolism and pharmacokinetics, toxicology, pharmaceutics and pharmacology, including proof-of-concept in the clinic for novel biological targets. The case studies include medicinal chemistry stories on recently approved and marketed drugs, but also chronicle "near-misses," i.e. exemplary compounds that may have proceeded well into the clinic but for various reasons did not result in a successful registration. As the vast majority of projects fail prior to registration, much can be learned from such narratives. By sharing a wide range of drug discovery experiences and information across the community of medicinal chemists in both industry and academia, the Editors believe that these accounts will provide insights into the art of medicinal chemistry as it is currently practiced and will help to serve the needs of active medicinal chemists.
Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section.
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
Computational methods are transforming the work of chemical and pharmaceutical laboratories. Increasingly faster and more exact simulation algorithms have made quantum chemistry a valuable tool in the search for active substances. Written by a team of leading international quantum chemists, this book is aimed at both beginners as well as experienced users of quantum chemical methods. All commonly used quantum chemical methods are treated here, including Density Functional Theory, quantum and molecular mechanical approaches. Numerous examples illustrate the use of these methods for dealing with problems in pharmaceutical practice, whether the study of inhibitor binding, identifying the surface load of active substances or deriving molecular descriptors using quantum chemical tools. For anyone striving to stay ahead in this rapidly evolving field.
Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations