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comprehensive medicinal chemistry ii free download: Practical Medicinal Chemistry with Macrocycles Eric Marsault, Mark L. Peterson, 2017-08-03 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 |
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comprehensive medicinal chemistry ii free download: Natural Products in Medicinal Chemistry Stephen Hanessian, 2013-12-18 The inspiration provided by biologically active natural products to conceive of hybrids, congeners, analogs and unnatural variants is discussed by experts in the field in 16 highly informative chapters. Using well-documented studies over the past decade, this timely monograph demonstrates the current importance and future potential of natural products as starting points for the development of new drugs with improved properties over their progenitors. The examples are chosen so as to represent a wide range of natural products with therapeutic relevance among others, as anticancer agents, antimicrobials, antifungals, antisense nucleosides, antidiabetics, and analgesics. From the content: * Part I: Natural Products as Sources of Potential Drugs and Systematic Compound Collections * Part II: From Marketed Drugs to Designed Analogs and Clinical Candidates * Part III: Natural Products as an Incentive for Enabling Technologies * Part IV: Natural Products as Pharmacological Tools * Part V: Nature: The Provider, the Enticer, and the Healer |
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comprehensive medicinal chemistry ii free download: Medicinal Chemistry of Bioactive Natural Products Xiao-Tian Liang, Wei-Shuo Fang, 2006-03-17 Current discoveries and research into bioactive natural products Medicinal Chemistry of Bioactive Natural Products provides a much-needed survey of bioactive natural products and their applications in medicinal chemistry. This comprehensive reference features articles by some of the world's leading scientists in the field on discovery, structure elucidation, and elegant synthetic strategies--developed for natural products--with an emphasis on the structure activity relationship of bioactive natural products. The topics have been carefully chosen on the basis of relevance to current research and to importance as clinicially useful agents. Rather than attempting to be a comprehensive encyclopedia of bioactive natural products, Medicinal Chemistry of Bioactive Natural Products guides the reader to the key developments in the field. By providing not only practical detail but a historical perspective on the chemistry and biology of the compounds under consideration, the book serves as a handy resource for researchers in their own work developing pharmaceuticals, and as an inspiring introduction for young scientists to the dynamic field of bioactive natural products research. Enhanced by examples with updated research results, the discussion covers such topics as: * The chemistry and biology of epothilones * Vancomycin and other glycopeptide antibiotic derivates * Antitumor and other related activities of Taxol and its analogs * The antimalarial properties of the traditional Chinese medicine, Quinghaosu (artemisinin) * Huperzine A: A natural drug for the treatment of Alzheimer's disease * The medicinal chemistry of ginkgolides from Ginkgo biloba * Recent progress in Calophyllum coumarins as potent anti-HIV agents * Plant-derived anti-HIV agents and analogs * Chemical synthesis of annonaceous acetogenins and their structurally modified mimics |
comprehensive medicinal chemistry ii free download: Quantum Medicinal Chemistry Paolo Carloni, Frank Alber, 2006-03-06 Computational methods are transforming the work of chemical and pharmaceutical laboratories. Increasingly faster and more exact simulation algorithms have made quantum chemistry a valuable tool in the search for active substances. Written by a team of leading international quantum chemists, this book is aimed at both beginners as well as experienced users of quantum chemical methods. All commonly used quantum chemical methods are treated here, including Density Functional Theory, quantum and molecular mechanical approaches. Numerous examples illustrate the use of these methods for dealing with problems in pharmaceutical practice, whether the study of inhibitor binding, identifying the surface load of active substances or deriving molecular descriptors using quantum chemical tools. For anyone striving to stay ahead in this rapidly evolving field. |
comprehensive medicinal chemistry ii free download: Fundamentals of Medicinal Chemistry and Drug Metabolism M. O. Faruk Khan, Ashok Philip, 2018-06-01 The primary objective of this 4-volume book series is to educate PharmD students on the subject of medicinal chemistry. The book set serves as a reference guide to pharmacists on aspects of chemical basis of drug action. This first volume of the series is comprised of 8 chapters focusing on basic background information about medicinal chemistry. It takes a succinct and conceptual approach to introducing important fundamental concepts required for a clear understanding of various facets of pharmacotherapeutic agents, drug metabolism and important biosynthetic pathways that are relevant to drug action. Notable topics covered in this first volume include the scope and importance of medicinal chemistry in pharmacy education, a comprehensive discussion of the organic functional groups present in drugs, and information about four major types of biomolecules (proteins, carbohydrates, lipids, nucleic acids) and key heterocyclic ring systems. The concepts of acid-base chemistry and salt formation, and their applications to the drug action and design follow thereafter. These include concepts of solubility and lipid-water partition coefficient (LWPC), isosterism, stereochemical properties, mechanisms of drug action, drug receptor interactions critical for pharmacological responses of drugs, and much more. Students and teachers will be able to integrate the knowledge presented in the book and apply medicinal chemistry concepts to understand the pharmacodynamics and pharmacokinetics of therapeutic agents in the body. |
comprehensive medicinal chemistry ii free download: Protein Crystallography in Drug Discovery, Volume 20 Robert E. Babine, Sherin S. Abdel-Meguid, 2004-02-13 The rational, structure-based approach has become standard in present-day drug design. As a consequence, the availability of high-resolution structures of target proteins is more often than not the basis for an entire drug development program. Protein structures suited for rational drug design are almost exclusively derived from crystallographic studies, and drug developers are relying heavily on the power of this method. Here, researchers from leading pharmaceutical companies present valuable first-hand information, much of it published for the first time. They discuss strategies to derive high-resolution structures for such important target protein classes as kinases or proteases, as well as selected examples of successful protein crystallographic studies. A special section on recent methodological developments, such as for high-throughput crystallography and microcrystallization, is also included. A valuable companion for crystallographers involved in protein structure determination as well as drug developers pursuing the structure-based approach for use in their daily work. |
comprehensive medicinal chemistry ii free download: Fluorine in Medicinal Chemistry and Chemical Biology Iwao Ojima, 2009-03-23 The extraordinary potential of fluorine-containing molecules in medicinal chemistry and chemical biology has been recognized by researchers outside of the traditional fluorine chemistry field, and thus a new wave of fluorine chemistry is rapidly expanding its biomedical frontiers. With several of the best selling drugs in the world crucially containing fluorine atoms, the incorporation of fluorine to drug leads has become an essential practice in biomedical research, especially for drug design and discovery as well as development. Focusing on the unique and significant roles that fluorine plays in medicinal chemistry and chemical biology, this book reviews recent advances and future prospects in this rapidly developing field. Topics covered include: Discovery and development of fluorine containing drugs and drug candidates. New and efficient synthetic methods for medicinal chemistry and the optimisation of fluorine-containing drug candidates. Structural and chemical biology of fluorinated amino acids and peptides. Fluorine labels as probes in metabolic study, protein engineering and clinical diagnosis. Applications of 19F NMR spectroscopy in biomedical research. An appendix presents an invaluable index of all fluorine-containing drugs that have been approved by the US Food and Drug Administration, including information on structure and pharmaceutical action. Fluorine in Medicinal Chemistry and Chemical Biology will serve as an excellent reference source for graduate students as well as academic and industrial researchers who want to take advantage of fluorine in biomedical research. |
comprehensive medicinal chemistry ii free download: Advances in Medicinal Chemistry B.E. Maryanoff, A.B. Reitz, 1999-04-01 Volume 4 of Advances in Medicinal Chemistry is comprised of six chapters on a wide range of topics in medicinal chemistry, including molecular modeling, structure-based drug design, organic synthesis, peptide conformational analysis, biological assessment, structure-activity correlation, and lead optimization. Chapter 1 presents an account about amino acid-based peptide mimetics corresponding to b-turn, loop, helical motifs in proteins as a probe of ligand-receptor and ligand-enzyme molecular interactions. Chapter 2 addresses new facets of the medicinal chemistry of the important anticancer drug Taxol® (paclitaxel). Chapter 3 relates an account of the search for new drugs for the treatment of malaria based on the natural product artemisinin. Chapter 4 applies computational chemistry to the evaluation of compound libraries for biological testing. Chapter 5 describes the construction of a 3-dimensional molecular model of the human thrombin receptor, the first protease-activated G-protein coupled receptor (PAR-1), as a means to explore the intermolecular contacts involved in agonist peptide recognition. Finally, Chapter 6 describes the research conducted at Merck on inhibitors of farnesyl transferase as a potential treatment for human cancers. |
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comprehensive medicinal chemistry ii free download: Antiviral Drug Strategies Erik De Clercq, 2011-04-08 By focusing on general molecular mechanisms of antiviral drugs rather than therapies for individual viruses, this ready reference provides the critical knowledge needed to develop entirely novel therapeutics and to target new viruses. It begins with a general discussion of antiviral strategies, followed by a broad survey of known viral targets, such as reverse transcriptases, proteases, neuraminidases, RNA polymerases, helicases and primases, as well as their known inhibitors. The final section contains several cases studies of recent successful antiviral drug development. Edited by Erik de Clercq, the world authority on small molecule antiviral drugs, who has developed more new antivirals than anyone else. |
comprehensive medicinal chemistry ii free download: The Organic Chemistry of Drug Design and Drug Action Richard B. Silverman, 2012-12-02 Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. - New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations - Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years - Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization |
comprehensive medicinal chemistry ii free download: Chemistry of Biologically Potent Natural Products and Synthetic Compounds Shahid Ul Islam, Javid Ahmad Banday, 2021-06-29 In view of their promising biological and pharmaceutical activities, natural product inspired and heterocyclic compounds have recently gained a reputation in the field of medicinal chemistry. Over the past decades, intensive research efforts have been ongoing to understand the synthesis, biochemistry and engineering involved in their preparation and action mechanisms. Several novel natural product derivatives, heterocyclic and other synthetic compounds, have been reported to have shown interesting biological activities including anticancer, antimicrobial, anti-inflammatory, anti-glycemic, anti-allergy and antiviral etc. Chemistry of Biologically Potent Natural Products and Synthetic Compounds provides up-to-date information on new developments and most recent medicinal applications of the natural products and derivatives, as well as the chemistry and synthesis of heterocyclic and other related compounds. |
comprehensive medicinal chemistry ii free download: High-Throughput Screening in Drug Discovery Jörg Hüser, 2006-12-13 Backed by leading authorities, this is a professional guide to successful compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for correct data evaluation. Chapter authors from leading pharmaceutical companies as well as from Harvard University discuss such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results. For both academics and professionals in the pharma and biotech industries working on small molecule screening. |
comprehensive medicinal chemistry ii free download: Medicinal Chemistry Gareth Thomas, 2011-09-20 Medicinal Chemistry: An Introduction, Second Edition provides a comprehensive, balanced introduction to this evolving and multidisciplinary area of research. Building on the success of the First Edition, this edition has been completely revised and updated to include the latest developments in the field. Written in an accessible style, Medicinal Chemistry: An Introduction, Second Edition carefully explains fundamental principles, assuming little in the way of prior knowledge. The book focuses on the chemical principles used for drug discovery and design covering physiology and biology where relevant. It opens with a broad overview of the subject with subsequent chapters examining topics in greater depth. From the reviews of the First Edition: It contains a wealth of information in a compact form ANGEWANDTE CHEMIE, INTERNATIONAL EDITION Medicinal Chemistry is certainly a text I would chose to teach from for undergraduates. It fills a unique niche in the market place. PHYSICAL SCIENCES AND EDUCATIONAL REVIEWS |
comprehensive medicinal chemistry ii free download: Comprehensive Medicinal Chemistry II: Drug discovery technologies , 2007 |
comprehensive medicinal chemistry ii free download: An Introduction to Medicinal Chemistry Graham L. Patrick, 2013-01-10 This volume provides an introduction to medicinal chemistry. It covers basic principles and background, and describes the general tactics and strategies involved in developing an effective drug. |
comprehensive medicinal chemistry ii free download: Medicinal Chemistry of Nucleic Acids Lihe Zhang, Zhen Xi, Jyoti Chattopadhyaya, 2011-08-10 Complete, up-to-date coverage of the broad area of nucleic acid chemistry and biology Assembling contributions from a collection of authors with expertise in all areas of nucleic acids, medicinal chemistry, and therapeutic applications, Medicinal Chemistry of Nucleic Acids presents a thorough overview of nucleic acid chemistry—a rapidly evolving and highly challenging discipline directly responsible for the development of antiviral and antitumor drugs. This reliable resource delves into a multitude of subject areas involving the study of nucleic acids—such as the new advances in genome sequencing, and the processes for creating RNA interference (RNAi) based drugs—to assist pharmaceutical researchers in removing roadblocks that hinder their ability to predict drug efficacy. Offering the latest cutting-edge science in this growing field, Medicinal Chemistry of Nucleic Acids includes: In-depth coverage of the development and application of modified nucleosides and nucleotides in medicinal chemistry A close look at a large range of current topics on nucleic acid chemistry and biology Essential information on the use of nucleic acid drugs to treat diseases like cancer A thorough exploration of siRNA for RNAi and the regulation of microRNA, non-coding RNA (ncRNA), a newly developing and exciting research area Thorough in its approach and promising in its message, Medicinal Chemistry of Nucleic Acids probes the new domains of pharmaceutical research—and exposes readers to a wealth of new drug discovery opportunities emerging in the dynamic field of nucleic acid chemistry. |
comprehensive medicinal chemistry ii free download: Lipophilicity in Drug Action and Toxicology Vladimir Pliska, Bernard Testa, Han van de Waterbeemd, 2008-09-26 In keeping with the outstanding importance of lipophilicity in biosciences, this volume examines all its facets in more than twenty contributions from leading experts. It offers a thorough and highly topical survey of this rapidly developing field of research. Color plates demonstrating structural aspects, a vast number of references, and the straightforward presentation of the material make this volume a invaluable tool for all researchers involved in drug design or in the investigation of drug action. |
comprehensive medicinal chemistry ii free download: Drug Selectivity Norbert Handler, 2018-02-27 The book Drug Selectivity - An Evolving Concept in Medicinal Chemistry provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process. The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist. |
comprehensive medicinal chemistry ii free download: Advanced Practical Medicinal Chemistry Ashutosh Kar, 2004 The Present Compendium On Advanced Practical Medicinal Chemistry Is Designed Specifically To Serve As A Text-Cum-Reference Book Not Only Intended For The Advanced Undergraduate And Graduate Students Of Pharmacy Specializing In Pharmaceutical Chemistry But Also For The Bulk-Drug Industrial Researchers And Academics Who Work Intimately With Medicinal Compounds. It Mainly Comprises Of Four Comprehensive Chapters. First Chapter Is Entirely Devoted To Safety In Chemical Laboratory, Which Is An Absolute Must For Each Medicinal Chemist. Second Chapter Is On Drug Synthesis And Concentrates On Three Vital Aspects, Namely : Conceptualization Of A Synthesis, Reaction Variants, And Stereochemistry. Third Chapter Exclusively Deals With Performing The Reactions And Entails The Wide Range Of Latest Laboratory Techniques Used In A Good Chemical Laboratory To Facilitate Synthesis Of Drugs.Fourth Chapter Is Particularly Focused And Earmarked To Synthesis Of Medicinal Compounds, And Essentially Include Various Cardinal Aspects, Such As :Types Of Chemical Reactions, Organic Name Reactions (Onrs), And Selected Medicinal Compounds. A Galaxy Of Eighty Carefully Chosen Medicinal Compounds Have Been Presented In Anoriginal-Unique-Style Comprising Of : Chemical Structure-Synonym (S)/Chemical Name(S)-Theory-Chemicals Required-Procedure-Precautions- Recrystallizatio-Theoretical Yield/Practical Yield-Physical Parameters-Uses, And -Questions For Viva-Voce.It Is Hoped That Advanced Practical Medicinal Chemistry Would Certainly Help To Bridge Existing Gap And Fill Up The Long Needed Vacuum In The Synthesis Of Drugs In Pharmaceutical Chemistry Departments, Academics And Bulk-Drug Industries, And May Provide The Basis For Meaningful Productive Group Discussions Of Synthetic Problems On A Broader Perspective. |
comprehensive medicinal chemistry ii free download: Comprehensive Medicinal Chemistry II: Computer-assisted drug design , 2007 |
comprehensive medicinal chemistry ii free download: Bioisosteres in Medicinal Chemistry Nathan Brown, 2012-10-15 Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section. |
comprehensive medicinal chemistry ii free download: Comprehensive Medicinal Chemistry II, Volume 1 John Bodenhan Taylor, D. J. Triggle, 2007 This e-book comprises 8 volumes, with all chapter sections available as PDF or HTML, and includes bibliographical references and index. |
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comprehensive medicinal chemistry ii free download: Carbohydrates as Drugs Peter H. Seeberger, Christoph Rademacher, 2014-11-14 Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors. |
comprehensive medicinal chemistry ii free download: Essentials of Inorganic Chemistry Katja A. Strohfeldt, 2015-02-16 A comprehensive introduction to inorganic chemistry and, specifically, the science of metal-based drugs, Essentials of Inorganic Chemistry describes the basics of inorganic chemistry, including organometallic chemistry and radiochemistry, from a pharmaceutical perspective. Written for students of pharmacy and pharmacology, pharmaceutical sciences, medicinal chemistry and other health-care related subjects, this accessible text introduces chemical principles with relevant pharmaceutical examples rather than as stand-alone concepts, allowing students to see the relevance of this subject for their future professions. It includes exercises and case studies. |
comprehensive medicinal chemistry ii free download: Comprehensive Medicinal Chemistry II: Strategy and drug research , 2007 |
comprehensive medicinal chemistry ii free download: Comprehensive Medicinal Chemistry II: Case histories and cumulative subject index , 2007 |
comprehensive medicinal chemistry ii free download: Comprehensive Medicinal Chemistry II, Volume 2 John Bodenhan Taylor, D. J. Triggle, 2007 This e-book comprises 8 volumes, with all chapter sections available as PDF or HTML, and includes bibliographical references and index. |
comprehensive medicinal chemistry ii free download: The ADME Encyclopedia Alan Talevi, 2022-06-14 The ADME Encyclopedia covers pharmacokinetic phenomena (Absorption, Distribution, Metabolism and Excretion processes) and their relationship with the design of pharmaceutical carriers and the success of drug therapies. It covers both basic and advanced knowledge, serving as introductory material for students of biomedical careers and also as reference, updated material for graduates and professionals working in any field related to pharmaceutical sciences (medicine, pharmaceutical technology, materials science, medicinal chemistry). Structured as alphabetically ordered entries with cross-references, the Encyclopedia not only provides basic knowledge on ADME processes, but also detailed entries on some advanced subjects such as drug transporters, last generation pharmaceutical carriers, pharmacogenomics, personalized medicine, bioequivalence studies, biowaivers, biopharmaceuticals, gene delivery, pharmacometrics, pharmacokinetic drug interactions or in silico and in vitro assessment of ADME properties |
comprehensive medicinal chemistry ii free download: Iptycenes Chemistry Chuan-Feng Chen, Ying-Xian Ma, 2012-12-02 Iptycenes Chemistry: From Synthesis to Applications provides a comprehensive overview of the development of iptycene chemistry in the past seventy years. This book covers: (1) the basic nomenclature and general properties of iptycenes and their derivatives; (2) the synthesis and functionalization reactions of triptycenes, pentiptycenes, higher iptycenes, heterotriptycenes, and homotriptycenes; (3) the methods for the preparation of iptycene-based polymers with different types; and (4) the applications of iptycenes and their derivatives in molecular machines, materials science, host-guest chemistry, self-assembly, coordination chemistry, physical organic chemistry, medicinal chemistry, and so on. Consequently, such a book is not only helpful to researchers working in iptycene chemistry, but can also facilitate future research in wide areas. |
comprehensive medicinal chemistry ii free download: Fragment-based Drug Discovery Daniel A. Erlanson, Wolfgang Jahnke, 2016-02-23 From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets. |
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