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The steroid scaffold continues to be the structural basis of new drugs for a variety of targets and diseases. Indeed, steroids interact with enzymes and receptors in a strikingly specific manner. Chemistry and Biological Activity of Steroids aims to provide an updated overview of recent advances in the medicinal chemistry of steroids. Novel synthetic methods in the steroids field, including steroid biotransformations, new steroids able to tackle steroid receptors, and steroid enzymes with clinical relevance, are critically reviewed in this book. Furthermore, the diverse physiopathological roles of oxysterols and their therapeutic value are also discussed.
The term steroid has become virtually synonymous with drug abuse in sport to the majority of the public. However these steroids - androgens - actually comprise only a single relatively small class of biologically active steroids, and are overshadowed by a large collection of compounds, a sizeable number of which are commercial drugs that share the same structural carbon skeleton. The development of these drugs has led to a large body of organic chemistry often denoted as "Steroid Chemistry". Steroid Chemistry At A Glance provides a concise overview of the main principles and reactions of steroid chemistry. Topics covered include: history, isolation and structure determination of steroids steroid nomenclature and stereochemistry natural sources of steroids synthesis and reactions of aromatic a-ring steroids, androstanes, and pregnanes steroids with a spirolactone at position 17 steroids with hetrocyclic ring A compounds derived from cholesterol Based on the highly successful and student friendly "at a glance" approach, the information is presented in integrated, self contained double page spreads of text and illustrative material. Students of chemistry and pharmacy using Steroid Chemistry at a Glance will find they have a resource with which they can quickly, concisely and confidently acquire, regularly review and revise the basic facts that underpin the properties, synthesis and reactions of this important class of natural products. It will also serve as a handy bench reference for postgraduates and professional chemists.
This volume provides comprehensive coverage of the current knowledge of the physiology of the endocrine system and hormone synthesis and release, transport, and action at the molecular and cellular levels. It presents essential as well as in-depth information of value to both medical students and specialists in Endocrinology, Gynecology, Pediatrics, and Internal Medicine. Although it is well established that the endocrine system regulates essential functions involved in growth, reproduction, and homeostasis, it is increasingly being recognized that this complex regulatory system comprises not only hormones secreted by the classic endocrine glands but also hormones and regulatory factors produced by many organs, and involves extensive crosstalk with the neural and immune system. At the same time, our knowledge of the molecular basis of hormone action has greatly improved. Understanding this complexity of endocrine physiology is crucial to prevent endocrine disorders, to improve the sensitivity of our diagnostic tools, and to provide the rationale for pharmacological, immunological, or genetic interventions. It is such understanding that this book is designed to foster.
This book is an essential reference guide to spectroscopic, physical and biological activity data of over 3500 steroid glycosides, offering the structures and the data of the naturally occurring glycosides of steroids. All compounds are arranged according to the structure of the aglycone, and, in its own class, by the increasing molecular weight, making Spectroscopic Data of Steroid Glycosides extremely useful for the structure elucidation of new natural products, particularly glycosides.
Molecular Structure and Biological Activity of Steroids focuses on the indentification of steroid structural features that control particular biological effects. Steroid geometry plays a critical role in steroid activity; therefore, the results of X-ray crystallographic, NMR spectroscopic, and theoretical studies on structure-activity relationships form an integral part of the book. Well-established observations and proposed models are presented, summarizing knowledge of molecular features (e.g., steroid backbone structures, side-chain constitutions, substitution sites, configurations, hydrogen-bonding patterns) that can affect steroid action. The book also provides overviews about recent progress in various frontier fields of steroid research, including such areas as sex steroids, glucocorticoids, aromatase inhibitors, vitamin D metabolites, brassinosteroids, neuromuscular blocking agents, and cardiotonic steroids. Molecular Structure and Biological Activity of Steroids is a "must-have" resource for biochemists, pharmacologists, endocrinologists, biophysicists, and others actively involved in steroid research.
Hormones provides a comprehensive treatment of human hormones viewed in the light of modern theories of hormone action and in the context of current understanding of subcellular and cellular architecture and classical organ physiology. The book begins with discussions of the first principles of hormone action and the seven classes of steroid hormones and their chemistry, biosynthesis, and metabolism. These are followed by separate chapters that address either a classical endocrine system, e.g., hypothalamic hormones, posterior pituitary hormones, anterior pituitary hormones, ,thyroid hormones, pancreatic hormones, gastrointestinal hormones, calcium regulating hormones, adrenal corticoids, hormones of the adrenal medulla, androgens, estrogens and progestins, and pregnancy and lactation hormones; or newer domains of hormone action which are essential to a comprehensive understanding of hormone action, including prostaglandins, thymus hormones, and pineal hormones. The book concludes with a presentation of hormones of the future, i.e., cell growth factors. This book is intended for use by first-year medical students, graduate students, and advanced undergraduates in the biological sciences. It is also hoped that this book will fill the void that exists for resource materials for teaching cellular and molecular endocrinology and that it will be employed as an equal partner with most standard biochemistry textbooks to provide a comprehensive and balanced coverage of this realm of biology.
This report on Future Trends in Inflammation IV records another of the multidisciplinary meetings organized by the European Biological Research Association. The organizers wish to record their thanks to all the participants and delegates who made this such an enjoyable meeting. Our thanks are due to a number of members of the pharmaceutical industry who so kindly donated funds. These funds were used to provide grants for young research workers to attend this meeting. Many people have kindly given their time and help to make this congress possible. It is impossible to list them by name, but we are profoundly grateful. We were dubious at the outset as to whether to hold this meeting in a period when many other meetings are being organized on inflammation. The enthusiastic attendance proves that we were right in going ahead. The next international meeting will be held in France in 1983. For further details please contact: Professor J. P. Giroud Department of Pharmacology, Hopital Cochin 75014 Paris, France D. A. Willoughby J. P. Giroud xxxiii Section I Future Trends CHAIRMAN: L. Chedid CO-CHAIRMAN: Dame Honor Fell 1 The participation of mononucleur phagocytes in immune based inflammatory processes with special reference to their secretory responses P. DAVIES AND R. J.
Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. - Serves as an essential working handbook aimed at scientists and students in medicinal chemistry - Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies - Discusses improvements in pharmacokinetics from a practical chemist's standpoint
Specialist Periodical Reports provide systematic and detailed review coverage of progress in the major areas of chemical research. Written by experts in their specialist fields the series creates a unique service for the active research chemist, supplying regular critical in-depth accounts of progress in particular areas of chemistry. For over 90 years The Royal Society of Chemistry and its predecessor, the Chemical Society, have been publishing reports charting developments in chemistry, which originally took the form of Annual Reports. However, by 1967 the whole spectrum of chemistry could no longer be contained within one volume and the series Specialist Periodical Reports was born. The Annual Reports themselves still existed but were divided into two, and subsequently three, volumes covering Inorganic, Organic and Physical Chemistry. For more general coverage of the highlights in chemistry they remain a 'must'. Since that time the SPR series has altered according to the fluctuating degree of activity in various fields of chemistry. Some titles have remained unchanged, while others have altered their emphasis along with their titles; some have been combined under a new name whereas others have had to be discontinued. The current list of Specialist Periodical Reports can be seen on the inside flap of this volume.
Synthesis of Essential Drugs describes methods of synthesis, activity and implementation of diversity of all drug types and classes. With over 2300 references, mainly patent, for the methods of synthesis for over 700 drugs, along with the most widespread synonyms for these drugs, this book fills the gap that exists in the literature of drug synthesis. It provides the kind of information that will be of interest to those who work, or plan to begin work, in the areas of biologically active compounds and the synthesis of medicinal drugs. This book presents the synthesis of various groups of drugs in an order similar to that traditionally presented in a pharmacology curriculum. This was done with a very specific goal in mind – to harmonize the chemical aspects with the pharmacology curriculum in a manner useful to chemists. Practically every chapter begins with an accepted brief definition and description of a particular group of drugs, proposes their classification, and briefly explains the present model of their action. This is followed by a detailed discussion of methods for their synthesis. Of the thousands of drugs existing on the pharmaceutical market, the book mainly covers generic drugs that are included in the WHO's Essential List of Drugs. For practically all of the 700+ drugs described in the book, references (around 2350) to the methods of their synthesis are given along with the most widespread synonyms. Synthesis of Essential Drugs is an excellent handbook for chemists, biochemists, medicinal chemists, pharmacists, pharmacologists, scientists, professionals, students, university libraries, researchers, medical doctors and students, and professionals working in medicinal chemistry. * Provides a brief description of methods of synthesis, activity and implementation of all drug types* Includes synonyms* Includes over 2300 references