Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists PDF Download
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Author: Koki Yamamoto Publisher: Springer Nature ISBN: 9811529655 Category : Science Languages : en Pages : 86
Book Description
This book explores the possible development of neurokinin-3 receptor (NK3R) antagonists with reduced environmental impact. Pharmaceuticals are used to cure diseases and to alleviate symptoms in humans and animals. However, the stable, bioactive substances excreted by patients have unfavorable effects on non-target species. To overcome these disadvantages of these highly stable, potent substances, drug design to turn off bioactivity after release into the environment is needed. The book describes the development of eco-friendly NK3R antagonists by introducing a labile functional moiety and substituting a scaffold. This resulted in a novel NK3R antagonist that oxidized into its inactive form when exposed to air. Further, the book presents an efficient and easily achievable synthetic method of creating triazolopiperazine scaffolds, as well as a structure–activity relationship study involving scaffold hopping for decomposable motifs, which led to a novel photodegradable NK3R antagonist. Demonstrating that it is possible to develop compounds that convert into their inactive forms under environmental conditions, this book is useful for anyone interested in therapeutic agents with reduced environmental impact.
Author: Koki Yamamoto Publisher: Springer Nature ISBN: 9811529655 Category : Science Languages : en Pages : 86
Book Description
This book explores the possible development of neurokinin-3 receptor (NK3R) antagonists with reduced environmental impact. Pharmaceuticals are used to cure diseases and to alleviate symptoms in humans and animals. However, the stable, bioactive substances excreted by patients have unfavorable effects on non-target species. To overcome these disadvantages of these highly stable, potent substances, drug design to turn off bioactivity after release into the environment is needed. The book describes the development of eco-friendly NK3R antagonists by introducing a labile functional moiety and substituting a scaffold. This resulted in a novel NK3R antagonist that oxidized into its inactive form when exposed to air. Further, the book presents an efficient and easily achievable synthetic method of creating triazolopiperazine scaffolds, as well as a structure–activity relationship study involving scaffold hopping for decomposable motifs, which led to a novel photodegradable NK3R antagonist. Demonstrating that it is possible to develop compounds that convert into their inactive forms under environmental conditions, this book is useful for anyone interested in therapeutic agents with reduced environmental impact.
Author: Veronique Gouverneur Publisher: World Scientific ISBN: 1908977892 Category : Science Languages : en Pages : 571
Book Description
Fluorine chemistry is an expanding area of research that is attracting international interest, due to the impact of fluorine in drug discovery and in clinical and molecular imaging (e.g. PET, MRI). Many researchers and academics are entering this area of research, while scientists in industrial and clinical environments are also indirectly exposed to fluorine chemistry through the use of fluorinated compounds for imaging.This book provides an overview of the impact that fluorine has made in the life sciences. In the first section, the emphasis is on how fluorine substitution of amino acids, peptides, nucleobases and carbohydrates can provide invaluable information at a molecular level. The following chapters provide answers to the key questions posed on the importance of fluorine in drug discovery and clinical applications. For examples, the reader will discover how fluorine has found its place as a key element improving drug efficacy, with reference to some of the best-selling drugs on the market. Finally, a thorough review on the design, synthesis and use of 18F-radiotracers for positron emission tomography is provided, and this is complemented with a discussion on how 19F NMR has advanced molecular and clinical imaging./a
Author: Mariana Spetea Publisher: MDPI ISBN: 3036500464 Category : Medical Languages : en Pages : 358
Book Description
The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general.
Author: Publisher: Elsevier ISBN: 0444634851 Category : Science Languages : en Pages : 314
Book Description
Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume includes chapters covering recent advances in cancer therapeutics, fluorine in medicinal chemistry, a perspective on the next generation of antibacterial agents derived by manipulation of natural products, a new era for Chagas Disease drug discovery? and imaging in drug development. Extended timely reviews of topics in medicinal chemistry Targets and technologies relevant to the discovery of tomorrow’s drugs Analyses of successful drug discovery programmes
Author: Terry W. Moody Publisher: Springer Science & Business Media ISBN: 1468451529 Category : Medical Languages : en Pages : 713
Book Description
The Fifth Annual Washington Spring Symposium on Health Sciences attracted over 400 scientists from 20 countries. It was held at the Lisner Auditorium of the George Washington University in Washington. D.C. The theme of the meeting was neural and endocrine peptides and receptors. The meeting emphasized basic and clinical research on neural and endocrine peptides and receptors. The six plenary sessions emphasized pituitary peptides, releasing factors, brain peptides, growth factors, peripheral peptides, and clinical applications. The chapters in this volume are derived from each of these six scientific sessions plus the poster and special sessions. The Abraham White Distinguished Scientist A ward was presented to Dr. Julius Axelrod for his numerous contributions to the field of neurochemistry. He presented the keynote address, which was entitled "The Regulation of the Release of ACTH." Dr. Axelrod discussed numerous factors, such as the peptides CRF, VIP, and somatostatin, that regulate hormone secretion from pituitary cells. The Distinguished Public Service Award was presented to Senator Lowell Weicker, Jr., in recognition of his leadership and outstanding achievements in the United States Senate and for his legislative support for biomedical research and education. In the symposium banquet address, Senator Weicker stressed the need for continued federal support of biomedical science research.
Author: Hirokazu Tamamura Publisher: Springer ISBN: 981107691X Category : Science Languages : en Pages : 113
Book Description
This brief describes studies conducted by the authors on mid-size drugs utilizing peptides and peptidomimetics, and on the development of anti-HIV agents. Peptides are important biological molecules and have various physiological actions. Peptide-based drug discovery may help bring about the development of useful medicines that are highly safe and show potent pharmacological effects in small doses. Recently, it has been shown that there is an important drug-like space in the mid-sized region between low- and high-molecular-weight compounds. Thus, mid-size drugs such as peptide compounds are being focused on. To date, several peptidomimetics that mimic primary, secondary, and tertiary structures of peptides have been developed to maintain and improve biological activities and actions of peptides. In this book, the features and advantages of mid-size drugs are described in detail. In addition, the merits of utilizing peptidomimetics in the development of mid-size drugs are referred to. Understanding such peptide-derived mid-size drugs will lead to a comprehensive expansion of medicinal chemistry.
Author: Manfred E. Wolff Publisher: Wiley-Interscience ISBN: 9780471575603 Category : Science Languages : en Pages : 904
Book Description
The final volume in the standard-setting reference on therapeutic designed drugs . . . BURGER'S MEDICINAL CHEMISTRY AND DRUG DISCOVERY, FIFTH EDITION, Volume 5: Therapeutic Agents This volume on Therapeutic Agents completes Burger's incisive, systematic examination of the fascinating new world of custom-designed therapeutic agents. Volume 5 highlights the link between chemical structure and biological activity, and explores chemotherapeutic agents, CNS and endocrine drugs, and radiological agents. It continues the authoritative coverage begun in earlier volumes and contains a comprehensive index for the entire edition. * Antimalarial agents * Agents affecting the action of * Cognition enhancers, agents, and prostaglandins pharmacodynamic models for * Agents affecting the action of Alzheimer's disease leukotrienes and thromboxanes * Antidepressant agent * Histamine H1 receptor antagonists * Antianxiety agents * Antiviral agents, RNA viruses * Antipsychotic agents other than HIV * Antihistamines, topical ocular * Radiopaques * Antiinflammatory steroids Essential to research in drug discovery and design, Volume 5 of Burger's Medicinal Chemistry and Drug Discovery is a cornerstone reference for professionals in the biopharmaceutical industry and academic research. Burger's Medicinal Chemistry, Fifth Edition consists of five volumes: * Volume 1: Principles and Practice (0-471-57556-9) 1994 * ". . . an essential addition to the libraries of any medicinal chemist . . . an outstanding work . . . highly praised as a fountain of information in drug studies and research."--Journal of Medicinal Chemistry * Volume 2: Therapeutic Agents (0-471-57557-7) 1996 * Volume 3: Therapeutic Agents (0-471-57558-5) 1996 * Volume 4: Therapeutic Agents (0-471-57559-3) 1997 * Volume 5: Therapeutic Agents (0-471-57560-7) 1997
Author: Stephen H. Buck Publisher: Springer Science & Business Media ISBN: 1461203015 Category : Medical Languages : en Pages : 637
Book Description
Offers a state-of-the-art review by international experts on all aspects of tachykinin receptors, including neuropeptide/peptide and G-protein-linked receptors in general. It covers the physiology, pharmacology, biochemistry, and molecular biology of these receptors from both clinical and basic research points of view. Topics treated by the distinguished contributors include the characterization of tachykinin receptors, the mechanisms of tachykinin receptor action, a reflection on future prospects, and a historical consideration of tachykinin research.
Author: Koki Yamamoto
Author: Koki Yamamoto
Author: Veronique Gouverneur
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Author: 
Author: Mariana Spetea
Author: 
Author: Terry W. Moody
Author: Hirokazu Tamamura
Author: Manfred E. Wolff
Author: Stephen H. Buck