This book brings together the theoretical, commercial, and practical aspects of chirality and biological activity of drugs and acts as a ready reference for the effects of enantiomers of drug substances.

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 characterist

This title was first published in 2001: In the early twentieth century the relevance of chirality to the pharmaceutical industry was established by the fact that one enantiomer of hyoscyamine possessed greater pharmacological activity than the other. Today, most new drugs and those under development consist of a single optically active isomer, and chirality is also becoming an issue for the agrochemical and other industries. Regulatory agencies throughout the world are currently reviewing the importance of chirality with regard to pharmaceutical and agrochemical products. New guidelines from such agencies have been key drivers for the focus on single enantiomer products in these industries. These scientific and regulatory developments have created the need for a guide for workers in the pharmaceutical and chemical industries seeking information on chiral molecules, processes, and commercially available chiral chemicals. Chiral Drugs is a comprehensive listing of over 2500 chiral drugs, classified by therapeutic class, and including structures and physical properties for each entry in the listing. Its companion volume, Chiral Intermediates, presents the same detailed information for over 4700 commercially available chiral chemicals. The 'Chiral Pool' of readily available, relatively inexpensive chiral compounds has been expanding at a rapid rate as more and more products are produced in large quantities at economical prices. New developments in various technologies for isolating, preparing, and purifying chiral materials have greatly increased the opportunities for utilizing optically pure compounds in commercial applications. Novel techniques for classical resolution, new methodologies for developing selective enzymes for biocatalysis, advances in the application of microorganisms for chemical production, and continued progress in the area of asymmetric synthesis have all contributed to the growth of this field. Part One of each book contains four chapters which provide an introduction to topics relevant to the field of chiral chemistry and includes a brief overview of chirality, a short discussion on the current market drivers in the area of chiral chemistry, and a basic presentation of the various sources and methods for obtaining chiral compounds. Part Two presents entries for over 2500 chiral drugs, classified by therapeutic class. For each main entry, the chemical name and a list of trade names and synonyms is provided; the CAS Registry Number, the European Inventory of Existing Commercial Chemical Substances (EINECS) number, and the Merck Index (12th edition) number are given when available. The physical properties, including specific rotation, of each compound are described and indicated applications are presented. The structure of nearly every compound is provided, and the manufacturers and suppliers of the compounds are also given. Indexes, including a master index of names and synonyms and an index of custom manufacturing services for production of chiral compounds, are appended. Chiral Drugs provides an introduction to the types of sources and methods currently in use for obtaining chiral molecules and is an invaluable resource for researchers in the pharmaceutical and biotechnology sectors as well as to those working in the basic biochemical sciences. Chiral Intermediates provides an introduction to the types of sources and methods currently in use for obtaining chiral molecules and is an invaluable resource for information on available chiral molecules. Chiral Intermediates and Chiral Drugs are the most comprehensive and detailed guides to chiral compounds available.

The book Alkaloids - Alternatives in Synthesis, Modification, and Application collects several chapters written by distinguished scientists and recognized experts in their respective fields of research. The purpose of this book is to focus the attention of a broad range of students, researchers, and specialists on some innovative and highly perspective areas in alkaloid research. The book covers several topics, guiding the readers from the development of nonconventional biotechnologies for alternative production of valuable alkaloids, through the application of modern chemical methods of asymmetric synthesis for production of synthetic and semisynthetic alkaloid derivatives, medicinal application of alkaloids as anesthetics and pain-relief drugs, analytical techniques for alkaloid profiling and their application in chemotaxonomy, quality control and standardization of raw plant material, to the importance of the control and reduction of alkaloid contents during production of animal feedstuffs.

Phosphorus Chemistry Directed Towards Biology presents an understanding of reaction mechanisms of organophosphorus compounds. This book discusses the development of analytical tools for the study of the chemistry of phosphorus, which promoted research in nucleic acid chemistry. Organized into 22 chapters, this book begins with an overview of the importance of the bacterial cell wall in maintaining the integrity of the cell in various environments. This text then examines the chemical problems concerning hypermodification and deprotection steps. Other chapters consider the reactive phosphorylating intermediates used in the oligonucleotide chemistry. This book discusses as well the possible role of phosphodiester triazolides and tetrazolides in the phosphotriester formation with arenesulfonyltriazolides and tetrazolides. The final chapter deals with the isolation of proteins involved in the synthesis and recognition of mRNA caps. This book is a valuable resource for phosphorus chemists, biologists, scientists, research workers, teachers, and students.

Although the United States (U.S.) and the more developed nations of the remainder of the world are blessed with a variety of pharmaceuticals, feed additives, and biological products to treat, prevent, and control animal diseases, there is a healthy desire among persons involved in animal health issues to increase our animal medicine chest. The interest stems from the desire to efficiently produce food that is safe and plentiful and from the desire to have more and better government-approved products available for the prevention and treatment of diseases of dogs, cats, and horses and for an increasing variety of minor animal species. For the animal health industry, increased drug availability means broader markets, increased revenues, and an opportunity to better serve their customers. For the veterinarian, more animal health products means that he or she is better able to treat the usual and the unusual conditions, and to prevent animal disease and suffering. No doubt, we are all winners when new technology and industrial and regulatory initiatives hasten the availability of safe and effective animal health products.

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.

Chirality is a concept related not only to organic chemistry but also to each field of natural science. Awareness of hierarchy is important for universal and comprehensive understanding. As such, this book examines myriad subjects related to chirality in chemistry and interdisciplinary applications. In contrast to the previous book, this new book about chirality includes contributions from authors in many fields of natural science, providing a wider overview. The book’s focus is chirality and organic chemistry, including synthesis and reactions.

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.

Although many books exist on the subject of chiral chemistry, they only briefly cover chiral synthesis and analysis as a minor part of a larger work, to date there are none that pull together the background information and latest advances in one comprehensive reference work. Comprehensive Chirality provides a complete overview of the field, and includes chiral research relevant to synthesis, analytic chemistry, catalysis, and pharmaceuticals. The individual chapters in each of the 9 volumes provide an in depth review and collection of references on definition, technology, applications and a guide/links to the related literature. Whether in an Academic or Corporate setting, these chapters will form an invaluable resource for advanced students/researchers new to an area and those who need further background or answers to a particular problem, particularly in the development of drugs. Chirality research today is a central theme in chemistry and biology and is growing in importance across a number of disciplinary boundaries. These studies do not always share a unique identifying factor or subject themselves to clear and concise definitions. This work unites the different areas of research and allows anyone working or researching in chiral chemistry to navigate through the most essential concepts with ease, saving them time and vastly improving their understanding. The field of chirality counts several journals that are directly and indirectly concerned with the field. There is no reference work that encompasses the entire field and unites the different areas of research through deep foundational reviews. Comprehensive Chirality fills this vacuum, and can be considered the definitive work. It will help users apply context to the diverse journal literature offering and aid them in identifying areas for further research and/or for solving problems. Chief Editors, Hisashi Yamamoto (University of Chicago) and Erick Carreira (ETH Zürich) have assembled an impressive, world-class team of Volume Editors and Contributing Authors. Each chapter has been painstakingly reviewed and checked for consistent high quality. The result is an authoritative overview which ties the literature together and provides the user with a reliable background information and citation resource.