Chirality and Biological Activity of Drugs


Book Description

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.




Chiral Drugs


Book Description

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 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.




Chirality and Biological Activity


Book Description

Reporting on the latest advances in molecular asymmetry, it explores the development of stereochemical analysis and its applications to the biosciences. Applications to pharmacology and therapeutics, food and beverage chemistry, the study of pesticides and other zenobiotics are also covered. Chapters examine the molecular principles of chiral recognition and biological selectivity and discuss stereoselectivity in drug action and metabolism. Some of the specific issues covered include: gas and liquid chromatography of enantiomers on chiral stationary phases; stereochemical assays of chiral drugs; pyrethroid isomers; configurational modification of peptide hormones; chiral fruit flavors; and human pharmacokinetics of enantiomers administered as racemates.




Chirality in Drug Design and Synthesis


Book Description

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


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.




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 characterist




Chiral Liquid Chromatography


Book Description

While working as a chromatographer in the pharmaceutical industry, it became apparent to the editor that there was a pressing need for a comprehensive reference text for analysts working on the resolution of enantiomers by liquid chromatography (LC). This need arises from the fact that, whereas previously it was very difficult to determine enantiomers by direct means, there is now a wide choice of direct LC methods. At the same time, regulatory authorities have been changing their attitudes towards the administration of pharmaceuticals as racemates, partly because it is now possible to study the individual enantiomers. Clearly this abundance of new information needs to be rationalized. More importantly, the chiral LC systems which are commercially available or readily accessible to the practising chromatographer needed to be reviewed and, to a much greater extent than in existing reviews or books, discussed in terms of their practical application. Accordingly this book is very much orientated towards the practical aspects of these commercially available and readily accessible chiral LC systems. To this end, it is written for practising chromatographers by a team of practising, experienced chromatographers who have spent many years tackling the problems presented by resolving enantiomers by LC. The practical aspects of common chiral LC systems cannot be fully understood if discussed in isolation.




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.




“What you need to know about Chiral Drugs: Nomenclature, Pharmacology, Mechanisms, Metabolism, Toxicology etc. An Overview.’’


Book Description

Approximately more than half of the drugs recently/currently in use are chiral compounds and near 90% of the last ones are marketed as racemates consisting of an equimolar mixture of two enantiomers. Although they have the same chemical structure, most isomers of chiral drugs exhibit marked differences in biological activities such as: · Pharmacology, · Toxicology, · Pharmacokinetics, · Metabolism etc. Therefore, it is important to promote the chiral separation and analysis of racemic drugs in pharmaceutical industry as well as in clinic in order to eliminate the unwanted isomer from the preparation and to find an optimal treatment and a right therapeutic control for the patient. An attempt has been made to review the nomenclature, pharmacology, toxicology, pharmacokinetics, metabolism etc. of some usual chiral drugs as well as their mechanisms of these properties. Additionally, different techniques used for the chiral separation in pharmaceutical industry as well as in clinical analyses have also been considered. …….Dr.H.K.Saboowala.M.B.(Bom) M.R.S.H.(London)