Structure Activity Relationships For Development Of Neurokinin 3 Receptor Antagonists

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Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists

Author : Koki Yamamoto
Publisher : Springer Nature
ISBN 13 : 9811529655
Total Pages : 86 pages
Book Rating : 4.8/5 (115 download)

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Book Synopsis Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists by : Koki Yamamoto

Download or read book Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists written by Koki Yamamoto and published by Springer Nature. This book was released on 2020-01-23 with total page 86 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Fluorine In Pharmaceutical And Medicinal Chemistry: From Biophysical Aspects To Clinical Applications

Author : Veronique Gouverneur
Publisher : World Scientific
ISBN 13 : 1908977892
Total Pages : 571 pages
Book Rating : 4.9/5 (89 download)

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Book Synopsis Fluorine In Pharmaceutical And Medicinal Chemistry: From Biophysical Aspects To Clinical Applications by : Veronique Gouverneur

Download or read book Fluorine In Pharmaceutical And Medicinal Chemistry: From Biophysical Aspects To Clinical Applications written by Veronique Gouverneur and published by World Scientific. This book was released on 2012-04-26 with total page 571 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Cumulated Index Medicus

Author :
Publisher :
ISBN 13 :
Total Pages : 1764 pages
Book Rating : 4.3/5 (243 download)

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Book Synopsis Cumulated Index Medicus by :

Download or read book Cumulated Index Medicus written by and published by . This book was released on 2000 with total page 1764 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Index Medicus

Author :
Publisher :
ISBN 13 :
Total Pages : 1938 pages
Book Rating : 4.:/5 (319 download)

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Book Synopsis Index Medicus by :

Download or read book Index Medicus written by and published by . This book was released on 2004 with total page 1938 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vols. for 1963- include as pt. 2 of the Jan. issue: Medical subject headings.

Opioids and Their Receptors

Author : Mariana Spetea
Publisher : MDPI
ISBN 13 : 3036500464
Total Pages : 358 pages
Book Rating : 4.0/5 (365 download)

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Book Synopsis Opioids and Their Receptors by : Mariana Spetea

Download or read book Opioids and Their Receptors written by Mariana Spetea and published by MDPI. This book was released on 2020-12-18 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Progress in Medicinal Chemistry

Author :
Publisher : Elsevier
ISBN 13 : 0444634851
Total Pages : 314 pages
Book Rating : 4.4/5 (446 download)

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Book Synopsis Progress in Medicinal Chemistry by :

Download or read book Progress in Medicinal Chemistry written by and published by Elsevier. This book was released on 2015-02-02 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Neural and Endocrine Peptides and Receptors

Author : Terry W. Moody
Publisher : Springer Science & Business Media
ISBN 13 : 1468451529
Total Pages : 713 pages
Book Rating : 4.4/5 (684 download)

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Book Synopsis Neural and Endocrine Peptides and Receptors by : Terry W. Moody

Download or read book Neural and Endocrine Peptides and Receptors written by Terry W. Moody and published by Springer Science & Business Media. This book was released on 2013-04-17 with total page 713 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Mid-size Drugs Based on Peptides and Peptidomimetics

Author : Hirokazu Tamamura
Publisher : Springer
ISBN 13 : 981107691X
Total Pages : 113 pages
Book Rating : 4.8/5 (11 download)

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Book Synopsis Mid-size Drugs Based on Peptides and Peptidomimetics by : Hirokazu Tamamura

Download or read book Mid-size Drugs Based on Peptides and Peptidomimetics written by Hirokazu Tamamura and published by Springer. This book was released on 2018-01-16 with total page 113 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Burger's Medicinal Chemistry and Drug Discovery, Therapeutic Agents

Author : Manfred E. Wolff
Publisher : Wiley-Interscience
ISBN 13 : 9780471575603
Total Pages : 904 pages
Book Rating : 4.5/5 (756 download)

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Book Synopsis Burger's Medicinal Chemistry and Drug Discovery, Therapeutic Agents by : Manfred E. Wolff

Download or read book Burger's Medicinal Chemistry and Drug Discovery, Therapeutic Agents written by Manfred E. Wolff and published by Wiley-Interscience. This book was released on 1997-04-24 with total page 904 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

The Tachykinin Receptors

Author : Stephen H. Buck
Publisher : Springer Science & Business Media
ISBN 13 : 1461203015
Total Pages : 637 pages
Book Rating : 4.4/5 (612 download)

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Book Synopsis The Tachykinin Receptors by : Stephen H. Buck

Download or read book The Tachykinin Receptors written by Stephen H. Buck and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 637 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Current Medicinal Chemistry

Author :
Publisher :
ISBN 13 :
Total Pages : 86 pages
Book Rating : 4./5 ( download)

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Book Synopsis Current Medicinal Chemistry by :

Download or read book Current Medicinal Chemistry written by and published by . This book was released on 1999-05 with total page 86 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Cambridge Scientific Biochemistry Abstracts

Author :
Publisher :
ISBN 13 :
Total Pages : 678 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis Cambridge Scientific Biochemistry Abstracts by :

Download or read book Cambridge Scientific Biochemistry Abstracts written by and published by . This book was released on 1992 with total page 678 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Rang & Dale's Pharmacology

Author : James M. Ritter
Publisher : Elsevier Health Sciences
ISBN 13 : 0702054976
Total Pages : 785 pages
Book Rating : 4.7/5 (2 download)

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Book Synopsis Rang & Dale's Pharmacology by : James M. Ritter

Download or read book Rang & Dale's Pharmacology written by James M. Ritter and published by Elsevier Health Sciences. This book was released on 2014-12-02 with total page 785 pages. Available in PDF, EPUB and Kindle. Book excerpt: For 25 years, Rang and Dale’s Pharmacology has delivered the core basic and clinical science information required by students and healthcare practitioners worldwide. Authors H. P. Rang, J. M. Ritter, R. J. Flower, and G. Henderson have ensured that the 8th Edition of this easy-to-read, comprehensive text continues the tradition of excellence with new coverage of drugs affecting the skin and new components online at studentconsult.com. Consult this title on your favorite e-reader. Get the essential pharmacology information you need from one authoritative source with an outstanding global reputation for excellence. Progress confidently through all relevant aspects of pharmacology, beginning with a molecular understanding of receptors and drug actions through clinical uses of key groups of drugs. Find important content quickly thanks to a color-coded layout that enables easy navigation and cross-referencing. Master difficult concepts with Key Points boxes, Clinical Uses boxes, and full-color illustrations throughout. Stay up to date with new information in the field, including an all-new chapter on drugs that affect the skin. Take advantage of new and unique features online, including 500+ chapter-specific multiple choice questions for immediate self-assessment. eBook version included! For the first time, you can access the entire book online or offline across all devices with the Student Consult eBook!

Drug-like Properties: Concepts, Structure Design and Methods

Author : Li Di
Publisher : Elsevier
ISBN 13 : 0080557619
Total Pages : 549 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Drug-like Properties: Concepts, Structure Design and Methods by : Li Di

Download or read book Drug-like Properties: Concepts, Structure Design and Methods written by Li Di and published by Elsevier. This book was released on 2010-07-26 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Burger's Medicinal Chemistry, Drug Discovery and Development, 8 Volume Set

Author :
Publisher : John Wiley & Sons
ISBN 13 : 111953030X
Total Pages : 6057 pages
Book Rating : 4.1/5 (195 download)

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Book Synopsis Burger's Medicinal Chemistry, Drug Discovery and Development, 8 Volume Set by :

Download or read book Burger's Medicinal Chemistry, Drug Discovery and Development, 8 Volume Set written by and published by John Wiley & Sons. This book was released on 2021-04-20 with total page 6057 pages. Available in PDF, EPUB and Kindle. Book excerpt: Burger’s Medicinal Chemistry, Drug Discovery and Development Explore the freshly updated flagship reference for medicinal chemists and pharmaceutical professionals The newly revised eighth edition of the eight-volume Burger’s Medicinal Chemistry, Drug Discovery and Development is the latest installment in this celebrated series covering the entirety of the drug development and discovery process. With the addition of expert editors in each subject area, this eight-volume set adds 35 chapters to the extensive existing chapters. New additions include analyses of opioid addiction treatments, antibody and gene therapy for cancer, blood-brain barrier, HIV treatments, and industrial-academic collaboration structures. Along with the incorporation of practical material on drug hunting, the set features sections on drug discovery, drug development, cardiovascular diseases, metabolic diseases, immunology, cancer, anti-Infectives, and CNS disorders. The text continues the legacy of previous volumes in the series by providing recognized, renowned, authoritative, and comprehensive information in the area of drug discovery and development while adding cutting-edge new material on issues like the use of artificial intelligence in medicinal chemistry. Included: Volume 1: Methods in Drug Discovery, edited by Kent D. Stewart Volume 2: Discovering Lead Molecules, edited by Kent D. Stewart Volume 3: Drug Development, edited by Ramnarayan S. Randad and Michael Myers Volume 4: Cardiovascular, Endocrine, and Metabolic Diseases, edited by Scott D. Edmondson Volume 5: Pulmonary, Bone, Immunology, Vitamins, and Autocoid Therapeutic Agents, edited by Bryan H. Norman Volume 6: Cancer, edited by Barry Gold and Donna M. Huryn Volume 7: Anti-Infectives, edited by Roland E. Dolle Volume 8: CNS Disorders, edited by Richard A. Glennon Perfect for research departments in the pharmaceutical and biotechnology industries, Burger’s Medicinal Chemistry, Drug Discovery and Development can be used by graduate students seeking a one-stop reference for drug development and discovery and deserves its place in the libraries of biomedical research institutes, medical, pharmaceutical, and veterinary schools.

CSA Neurosciences Abstracts

Author :
Publisher :
ISBN 13 :
Total Pages : 640 pages
Book Rating : 4.3/5 (91 download)

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Book Synopsis CSA Neurosciences Abstracts by :

Download or read book CSA Neurosciences Abstracts written by and published by . This book was released on 1996 with total page 640 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Drug-Like Properties

Author : Li Di
Publisher : Academic Press
ISBN 13 : 0128013222
Total Pages : 582 pages
Book Rating : 4.1/5 (28 download)

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Book Synopsis Drug-Like Properties by : Li Di

Download or read book Drug-Like Properties written by Li Di and published by Academic Press. This book was released on 2015-12-17 with total page 582 pages. Available in PDF, EPUB and Kindle. Book excerpt: Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, only a fraction have sufficient ADME (absorption, distribution, metabolism, elimination) properties, and acceptable toxicology properties, to become a drug product that will successfully complete human Phase I clinical trials. Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization, Second Edition, provides scientists and students the background and tools to understand, discover, and develop optimal clinical candidates. This valuable resource explores physiochemical properties, including solubility and permeability, before exploring how compounds are absorbed, distributed, and metabolized safely and stably. Review chapters provide context and underscore the importance of key concepts such as pharmacokinetics, toxicity, the blood-brain barrier, diagnosing drug limitations, prodrugs, and formulation. Building on those foundations, this thoroughly updated revision covers a wide variety of current methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties for process and product improvement. From conducting key assays for interpretation and structural analysis, the reader learns to implement modification methods and improve each ADME property. Through valuable case studies, structure-property relationship descriptions, and structure modification strategies, Drug-Like Properties, Second Edition, offers tools and methods for ADME/Tox scientists through all aspects of drug research, discovery, design, development, and optimization. Provides a comprehensive and valuable working handbook for scientists and students in medicinal chemistry Includes expanded coverage of pharmacokinetics fundamentals and effects Contains updates throughout, including the authors’ recent work in the importance of solubility in drug development; new and currently used property methods, with a reduction of seldom-used methods; and exploration of computational modeling methods