Download or read book Peptidomimetics in Organic and Medicinal Chemistry written by Antonio Guarna and published by John Wiley & Sons. This book was released on 2014-04-07 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt: A peptidomimetic is a small protein-like chain designed to mimic a peptide with adjusted molecular properties such as enhanced stability or biological activity. It is a very powerful approach for the generation of small-molecule-based drugs as enzyme inhibitors or receptor ligands. Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature. Topics covered include the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery.
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.
Download or read book Peptide and Peptidomimetic Therapeutics written by Nir Qvit and published by Academic Press. This book was released on 2022-09-22 with total page 792 pages. Available in PDF, EPUB and Kindle. Book excerpt: Peptide and Peptidomimetic Therapeutics: From Bench to Beside offers applied, evidence-based instruction on developing and applying peptide therapeutics in disease treatment, driving drug discovery, and improving patient care. Here, researchers, clinicians and students will find tools to harness the full power of peptides and peptidomimetics and improve bioavailability, stability, efficiency and selectivity of new therapeutics and their application in treatment plans. More than 20 leaders in the field share their approaches for identifying and advancing peptide and peptidomimetic therapeutics. Topics examined run from "bench to bedside," beginning with fundamental peptide science, protein-protein interactions and peptide synthesis. Later chapters examine modes for peptide drug delivery, including cell penetration peptide and peptidomimetic delivery, as well as the targeting of specific disease types, peptide therapeutics as applied to infectious disease, cancer, metabolic disorders, neurodegenerative disorders, and skin disorders, and antiparasitic and immunosuppressive peptidomimetics. - Helps researchers and clinicians harness the full of power of peptides and peptidomimetics in their daily work and drug discovery - Features chapters running from "bench to bedside, providing a thorough grounding in fundamental peptide science, drug delivery methods, and targeting of specific disease types - Features chapter contributions from international leaders in peptide science and drug development
Download or read book Small Molecule Medicinal Chemistry written by Werngard Czechtizky and published by John Wiley & Sons. This book was released on 2015-09-21 with total page 528 pages. Available in PDF, EPUB and Kindle. Book excerpt: Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs. • Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives • Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches • Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques • Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting
Download or read book Essentials of Organic Chemistry written by Paul M. Dewick and published by John Wiley & Sons. This book was released on 2013-03-20 with total page 711 pages. Available in PDF, EPUB and Kindle. Book excerpt: Essentials of Organic Chemistry is an accessible introduction to the subject for students of Pharmacy, Medicinal Chemistry and Biological Chemistry. Designed to provide a thorough grounding in fundamental chemical principles, the book focuses on key elements of organic chemistry and carefully chosen material is illustrated with the extensive use of pharmaceutical and biochemical examples. In order to establish links and similarities the book places prominence on principles and deductive reasoning with cross-referencing. This informal text also places the main emphasis on understanding and predicting reactivity rather than synthetic methodology as well as utilising a mechanism based layout and featuring annotated schemes to reduce the need for textual explanations. * tailored specifically to the needs of students of Pharmacy Medical Chemistry and Biological Chemistry * numerous pharmaceutical and biochemical examples * mechanism based layout * focus on principles and deductive reasoning This will be an invaluable reference for students of Pharmacy Medicinal and Biological Chemistry.
Download or read book Drug Design written by Gerhard Klebe and published by Springer. This book was released on 2013-07-10 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Unique work on structure-based drug design, covering multiple aspects of drug discovery and development. Fully colored, many images, computer animations of 3D structures (these only in electronic form). Makes the spatial aspects of interacting molecules clear to the reader, covers multiple applications and methods in drug design. Structures by mode of action, no therapeutic areas. Of high relevance for academia and industrial research. Focus on gene technology in drug design, omics-technologies computational methods experimental techniques of structure determination multiple examples on mode of action of current drugs, ADME-tox properties in drug development, QSAR methods, combinatorial chemistry, biologicals, ribosome, targeting protein-protein interfaces.
Download or read book Small Molecule Drug Discovery written by Andrea Trabocchi and published by Elsevier. This book was released on 2019-11-23 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: Small Molecule Drug Discovery: Methods, Molecules and Applications presents the methods used to identify bioactive small molecules, synthetic strategies and techniques to produce novel chemical entities and small molecule libraries, chemoinformatics to characterize and enumerate chemical libraries, and screening methods, including biophysical techniques, virtual screening and phenotypic screening. The second part of the book gives an overview of privileged cyclic small molecules and major classes of natural product-derived small molecules, including carbohydrate-derived compounds, peptides and peptidomimetics, and alkaloid-inspired compounds. The last section comprises an exciting collection of selected case studies on drug discovery enabled by small molecules in the fields of cancer research, CNS diseases and infectious diseases. The discovery of novel molecular entities capable of specific interactions represents a significant challenge in early drug discovery. Small molecules are low molecular weight organic compounds that include natural products and metabolites, as well as drugs and other xenobiotics. When the biological target is well defined and understood, the rational design of small molecule ligands is possible. Alternatively, small molecule libraries are being used for unbiased assays for complex diseases where a target is unknown or multiple factors contribute to a disease pathology. - Outlines modern concepts and synthetic strategies underlying the building of small molecules and their chemical libraries useful for drug discovery - Provides modern biophysical methods to screening small molecule libraries, including high-throughput screening, small molecule microarrays, phenotypic screening and chemical genetics - Presents the most advanced chemoinformatics tools to characterize the structural features of small molecule libraries in terms of chemical diversity and complexity, also including the application of virtual screening approaches - Gives an overview of structural features and classification of natural product-derived small molecules, including carbohydrate derivatives, peptides and peptidomimetics, and alkaloid-inspired small molecules
Download or read book Peptide based Drug Discovery written by Ved Srivastava and published by Royal Society of Chemistry. This book was released on 2017-06-26 with total page 589 pages. Available in PDF, EPUB and Kindle. Book excerpt: With potentially high specificity and low toxicity, biologicals offer promising alternatives to small-molecule drugs. Peptide therapeutics have again become the focus of innovative drug development efforts backed up by a resurgence of venture funds and small biotechnology companies. What does it take to develop a peptide-based medicine? What are the key challenges and how are they overcome? What are emerging therapeutics for peptide modalities? This book answers these questions with a holistic story from molecules to medicine, combining the themes of design, synthesis and clinical applications of peptide-based therapeutics and biomarkers. Chapters are written and edited by leaders in the field from industry and academia and they cover the pharmacokinetics of peptide therapeutics, attributes necessary for commercially successful metabolic peptides, medicinal chemistry strategies for the design of peptidase-resistant peptide analogues, disease classes for which peptide therapeutic are most relevant, and regulatory issues and guidelines. The critical themes covered provide essential background information on what it takes to develop peptide-based medicine from a chemistry perspective and views on the future of peptide drugs. This book will be a valuable resource not only as a reference book for the researcher engaged in academic and pharmaceutical setting, from basic research to manufacturing and from organic chemistry to biotechnology, but also a valuable resource to graduate students to understand discovery and development process for peptide-based medicine.
Download or read book Chemical Epigenetics written by Antonello Mai and published by Springer Nature. This book was released on 2020-03-31 with total page 569 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.
Download or read book Practical Medicinal Chemistry with Macrocycles written by Eric Marsault and published by John Wiley & Sons. This book was released on 2017-09-12 with total page 617 pages. Available in PDF, EPUB and Kindle. Book excerpt: Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations
Download or read book Introduction to Medicinal Chemistry written by Alex Gringauz and published by Wiley-VCH. This book was released on 1997 with total page 744 pages. Available in PDF, EPUB and Kindle. Book excerpt: This work brigdges the compartmentalized undergraduate organic and biochemistry and biology subjects to the pharmacology and the clinical areas a modern pharmacy practice requires. The changes and constantly increasing responsibilities of today's pharmacist have dictated a restructuring of the pharmacy curriculum, including individual course content. This book reflects and addresses these developments. This is a well-written work that covers most major areas of pharmaceutical research. The text is presented in a logical and concise fashion being divided into chapters based upon therapeutic topic. This makes the work very useful for teaching a course in medicinal chemistry since therapeutic areas can be separately covered without having to make use of the entire book which overall contains a tremendous amount of information. This book is a significant contribution to understanding what medicinal chemistry is and how this science is used to develop new therapeutic agents.
Download or read book Inhibitors of Protein Protein Interactions written by Ali Tavassoli and published by Royal Society of Chemistry. This book was released on 2020-12-07 with total page 357 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein-protein interactions (PPI) are at the heart of the majority of cellular processes, and are frequently dysregulated or usurped in disease. Given this central role, the inhibition of PPIs has been of significant interest as a means of treating a wide variety of diseases. However, there are inherent challenges in developing molecules capable of disrupting the relatively featureless and large interfacial areas involved. Despite this, there have been a number of successes in this field in recent years using both traditional drug discovery approaches and innovative, interdisciplinary strategies using novel chemical scaffolds. This book comprehensively covers the various aspects of PPI inhibition, encompassing small molecules, peptidomimetics, cyclic peptides, stapled peptides and macrocycles. Illustrated throughout with successful case studies, this book provides a holistic, cutting-edge view of the subject area and is ideal for chemical biologists and medicinal chemists interested in developing PPI inhibitors.
Download or read book Lead Optimization for Medicinal Chemists written by Florencio Zaragoza Dörwald and published by John Wiley & Sons. This book was released on 2013-02-04 with total page 627 pages. Available in PDF, EPUB and Kindle. Book excerpt: Small structural modifications can significantly affect the pharmacokinetic properties of drug candidates. This book, written by a medicinal chemist for medicinal chemists, is a comprehensive guide to the pharmacokinetic impact of functional groups, the pharmacokinetic optimization of drug leads, and an exhaustive collection of pharmacokinetic data, arranged according to the structure of the drug, not its target or indication. The historical origins of most drug classes and general aspects of modern drug discovery and development are also discussed. The index contains all the drug names and synonyms to facilitate the location of any drug or functional group in the book. This compact working guide provides a wealth of information on the ways small structural modifications affect the pharmacokinetic properties of organic compounds, and offers plentiful, fact-based inspiration for the development of new drugs. This book is mainly aimed at medicinal chemists, but may also be of interest to graduate students in chemical or pharmaceutical sciences, preparing themselves for a job in the pharmaceutical industry, and to healthcare professionals in need of pharmacokinetic data.
Download or read book Amino Acids Peptides and Proteins in Organic Chemistry written by Andrew B. Hughes and published by . This book was released on 2009 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Natural Products written by Raphael Ikan and published by Elsevier. This book was released on 2013-10-22 with total page 316 pages. Available in PDF, EPUB and Kindle. Book excerpt: This new edition has been updated to include the following: The use of biomarkers (organic compounds in the geospherical record with carbon skeletons) reflecting the upsurge in geoporphyrin research primarily due to MS, yeast RNA nucleic acid studies: reversed-phase HPLC of amino acids; brewing industry applications (HPLC evaluation of carotenoids in orange juice and of "debittered" citrus); HPTLC of carbohydrates; synthesis of a sweetening agent from citrus peels, synthesis and degradation of alkaloids and of sterols, GC/MS uses with sterols, petroleum products, and aromatic constituents of wine and grape juice, flash chromatography of essential oils, optical purity of enantiomers affecting flavors, fragrances, and pheromones, as well as studies of lattice inclusion compounds 1H- and 13C-NMR, MS, IR and UV data are presented for most natural products. Biomarkers—organic compounds in the geospherical record with carbon skeletons—reflecting the upsurge in geoporphyrin research primarily due to MS Yeast RNA nucleic acid studies Reversed-phase HPLC of amino acids, citrus juice components, and HPLC in brewing industry application HPTLC of carbohydrates 1H- and 13C-NMR: Sweetness evaluation and synthesis of a sweetening agent from citrus peels; seed oil sesamolin; alkaloids (strychnine, piperine, caffeine); and sterol analyses GC/MS: sterols, petroleum studies, aromatic constituents of wine and grapejuice Flash chromatography of essential oils Optical purity of enantiomers affecting flavors, fragrances, and pheromones Materials science studies of lattice inclusion compounds
Download or read book Development and Validation of Analytical Methods written by Christopher M. Riley and published by Elsevier. This book was released on 1996-05-29 with total page 363 pages. Available in PDF, EPUB and Kindle. Book excerpt: The need to validate an analytical or bioanalytical method is encountered by analysts in the pharmaceutical industry on an almost daily basis, because adequately validated methods are a necessity for approvable regulatory filings. What constitutes a validated method, however, is subject to analyst interpretation because there is no universally accepted industry practice for assay validation. This book is intended to serve as a guide to the analyst in terms of the issues and parameters that must be considered in the development and validation of analytical methods. In addition to the critical issues surrounding method validation, this book also deals with other related factors such as method development, data acquisition, automation, cleaning validation and regulatory considerations. The book is divided into three parts. Part One, comprising two chapters, looks at some of the basic concepts of method validation. Chapter 1 discusses the general concept of validation and its role in the process of transferring methods from laboratory to laboratory. Chapter 2 looks at some of the critical parameters included in a validation program and the various statistical treatments given to these parameters.Part Two (Chapters 3, 4 and 5) of the book focuses on the regulatory perspective of analytical validation. Chapter 3 discusses in some detail how validation is treated by various regulatory agencies around the world, including the United States, Canada, the European Community, Australia and Japan. This chapter also discusses the International Conference on Harmonization (ICH) treatment of assay validation. Chapters 4 and 5 cover the issues and various perspectives of the recent United States vs. Barr Laboratories Inc. case involving the retesting of samples. Part Three (Chapters 6 - 12) covers the development and validation of various analytical components of the pharmaceutical product development process. This part of the book contains specific chapters dedicated to bulk drug substances and finished products, dissolution studies, robotics and automated workstations, biotechnology products, biological samples, analytical methods for cleaning procedures and computer systems and computer-aided validation. Each chapter goes into some detail describing the critical development and related validation considerations for each topic.This book is not intended to be a practical description of the analytical validation process, but more of a guide to the critical parameters and considerations that must be attended to in a pharmaceutical development program. Despite the existence of numerous guidelines including the recent attempts by the ICH to be implemented in 1998, the practical part of assay validation will always remain, to a certain extent, a matter of the personal preference of the analyst or company. Nevertheless, this book brings together the perspectives of several experts having extensive experience in different capacities in the pharmaceutical industry in an attempt to bring some consistency to analytical method development and validation.
Download or read book Nanostructures for Novel Therapy written by Denisa Ficai and published by Elsevier. This book was released on 2017-02-25 with total page 908 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nanostructures for Novel Therapy: Synthesis, Characterization and Applications focuses on the fabrication and characterization of therapeutic nanostructures, in particular, synthesis, design, and in vitro and in vivo therapeutic evaluation. The chapters provide a cogent overview of recent therapeutic applications of nanostructured materials that includes applications of nanostructured materials for wound healing in plastic surgery and stem cell therapy. The book explores the promise for more effective therapy through the use of nanostructured materials, while also assessing the challenges their use might pose from both an economic and medicinal point of view. This innovative look at how nanostructured materials are used in therapeutics will be of great benefit to researchers, providing a greater understanding of the different ways nanomaterials could improve medical treatment, along with a discussion of the obstacles that need to be overcome in order to guarantee widespread availability. - Outlines how the characteristics of nanostructures made from different materials gives particular properties that can be successfully used in therapeutics - Compares the properties of different nanostructures, allowing medicinal chemists and engineers to select which are most appropriate for their needs - Highlights new uses of nanostructures within the therapeutic field, enabling the discovery of new, more effective drugs
