Progress in medicinal chemistry  v. 1 ~ v. 59

edited by G.P. Ellis and G.B. West

"The Progress in Medicinal Chemistry" series spans a wide range of topics of interest to the drug discovery community. This particular volume touches upon the following: the Herg ion channel; fluorescence-based high throughput assay; aprepitant and neurokinin receptors; muscarinic receptor targets; gene activation pathways; malaria and antimalarial drugs; and, HIV virus mutation and new therapeutics. "Progress in Medicinal Chemistry" is available online on ScienceDirect - full-text online of volumes 41 onwards. Elsevier book series on ScienceDirect gives multiple users throughout an institution simultaneous online access to an important compliment to primary research. Digital delivery ensures users reliable, 24-hour access to the latest peer-reviewed content. The Elsevier book series are compiled and written by the most highly regarded authors in their fields and are selected from across the globe using Elsevier's extensive researcher network. This title presents the latest research in the field of drug discovery. It publishes on an annual basis to bring you the most innovative updates in medicinal chemistry.

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Appropriate selection of biochemical targets is one of the most important drivers of cost effectiveness in the discovery of new medicines. Despite the many advances in genetics, genomics and systems biology, validation of a target is not achieved until therapeutic efficacy is demonstrated by a drug candidate.Volume 46 of this series reviews the medicinal chemistry aimed at six diverse targets from which important new medicines are emerging: HIV integrase (discovery of the first-in-class inhibitor drug raltegravir), 11-beta-Hydroxysteroid dehydrogenase (new approach to glucocorticoid regulation), nicotinic a7 choline receptor (agonists and positive allosteric modulators), bradykinin receptor (new approach to pain therapy); histone deacetylase (new drugs for cancer), and 5-HT2c receptor modulators (various CNS indications). This book presents the latest research in the field of drug discovery. It publishes on an annual basis to bring you the most innovative updates in medicinal chemistry. It is available as an online resource via ScienceDirect.

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Highlights of this volume include accounts of the biological rationale, design and clinical potential of drug molecules; summaries of structure-activity relationships in topical areas of medicinal chemistry; and evaluation of technologies in their application to drug action and design. The seven chapters describe advances in drug molecules and in the application of new technologies to drug discovery and development.

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Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems, including g-secretase modulators, P2X7 antagonists as therapeutic agents for CNS disorders, N-type calcium channel modulators for the treatment of pain, and more. * 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

「Nielsen BookData」より

Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems. *Presents the latest research in the field of drug discovery *Publishes on a twice yearly basis to bring you the most innovative updates in medicinal chemistry *Available as an online resource via ScienceDirect

「Nielsen BookData」より

Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems. *Presents the latest research in the field of drug discovery *Publishes on a twice yearly basis to bring you the most innovative updates in medicinal chemistry *Available as an online resource via ScienceDirect

「Nielsen BookData」より

Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems. Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry

「Nielsen BookData」より

Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems. Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems.

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The Progress in Medicinal Chemistry series is a respected and instructive source of information on the subject. It has a long established reputation for excellent coverage of almost every facet of medicinal chemistry. This volume includes information on the discovery and development of Atorvastatin; the discovery of CEP-1347/KT-7515, an JNK/SAPK pathway for the treatment of neurodegenerative diseases such; and the discovery of second generation Quinazolinone non-nucleoside reverse transcriptase inhibitors of HIV-1; and molecular modeling of Opioid receptor-Ligand complexes.

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The perceived lack of drug discovery productivity in recent times has led to much debate in the pharmaceutical/biotechnology industry as escalating R&D costs are not being matched by increased output. Few observers doubt that selecting the right targets, i.e, those which are critical to disease pathology and are druggable, is the best starting point for improved productivity. The seven chapters of this volume describe recent progress towards drugs acting at a range of druggable targets. One chapter addresses kinases, one covers an ion channel, two proteases are featured and three of the chapters cover G-protein coupled receptors, which has historically perhaps been the most fruitful area for medicinal chemists. It presents the latest research in the field of drug discovery. It publishes on an annual basis to bring you the most innovative updates in medicinal chemistry. It is available as an online resource via ScienceDirect.

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The six chapters presented in this volume review recent advances in important areas of medicinal chemistry. Chapter 1 describes the rational drug design of inhibitors of the influenza virus enzyme, sialidase, from which zanamivir was identified. This compound is representative of a new generation of agents for the treatment of human influenza infections. Nonpeptide small molecule fibrinogen antagonists are reviewed in chapter 2, indicating the extent of progress to identify compounds with good oral pharmacokinetics. The clinical trials of these potent antithrombotic agents are giving encouraging results in angioplasty and unstable angina and as an adjunct to thrombolysis therapy in myocardial infarction. Combinatorial chemistry, one of the most rapidly evolving techniques for drug discovery, is already the subject of many reviews but most are concerned with synthetic methodology. In contrast, chapter 3 considers the value of combinatorial chemistry to the medicinal chemist by reviewing the scope of its application to therapeutically important targets and reveals there is much progress to report. Advances in the molecular biology and pharmacology of the neurotransmitter, GABA, have established there is considerable heterogeneity in GABAa receptors, the receptors known to be modulated by all the clinically effective benzodiazepine anxiolytics. The consequent surge of activity to find anxiolytic agents which are more selective and possess fewer side-effects than the early benzodiazepines has led to the synthesis of a variety of novel structures. One such series of pyrido[1,2-a]benzimidazoles is described in chapter 4. There is good evidence to suggest that cyclooxygenase-2(COX-2) inhibitors will have important advantages over conventional non-steroidal anti-inflammatory drugs in arthritic disorders, and may be of value in Alzheimer's disease. The numerous compounds that exhibit COX-2 inhibitory activity are reviewed systematically in chapter 5. One of the most recent technologies to be developed is that of molecularly imprinted polymers. These materials have considerable potential in a variety of settings, including chromatographic separation of chiral molecules, and in the high throughput screening of complex mixtures such as combinatorial libraries. A survey of this field is given in chapter 6.

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The success of any drug discovery project relies upon the quality of the lead that initiates the lead optimization process. What defines a quality lead, where these quality leads come from and how one discovers them has been the subject of intense debate within the pharmaceutical industry, which relies upon defining those properties that historically have led to successful drug discovery. This volume addresses these questions and specifically discusses diabetes, obesity and tuberculosis. It presents the latest research in the field of drug discovery. It is published on an annual basis to bring you the most innovative updates in medicinal chemistry. It is available as an online resource via ScienceDirect.

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There are five main subject areas in this volume in the series on medicinal chemistry. The first is a review of the understanding of Alzheimer's disease and the development of drugs for its treatment; the second, looking at recent efforts in modifying a naturally occuring anticancer (campothecin) for chemotherapy; the third covers the problem of getting a drug to a specific site within the context of phosphates and phosphonates; a survey of sterilization using aldehydes for the destruction of microbes both inside and outside the human body is reviewed in the fourth; and the last chapter is an account of the progress made in the biologically active enantiomer for complex synthetic asymmetric drug molecules.

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This volume covers contemporary advances in five important areas of pharmacology and medicinal chemistry including: a comprehensive account of inhibitors of the caspase family of proteolytic enzymes that represent a new class of anti-inflammatory and antiapoptotic agents of potential value in rheumatoid arthritis, and other peripheral and central indications; adoc umented survey of semi-synthetic and totally synthetic antibiotics and anti HIV agents and their sites of interaction; inhibitors of the intracellular enzyme acyl-CoA: cholesterol O-acyltransferase (ACAT) developed for the treatment of hypercholesterolemia; and recent progress in growth hormone secretagogues, with the focus on strategies to improve oral bioavailability and duration of action. Inhibition of the proteolytic enzyme, hepatitis C protease N-3(NS3), required for viral replication, is one of the most attractive targets for HCV infections. Progress and prospects in the design of peptide and non-peptide inhibitors are described here. The book also contains comprehensive accounts of the biological rationale, design and clinical potential of new drug molecules; valuable summaries of structure-activity relationships in topical areas of medicinal chemistry; and extensive references to the biology, medicinal chemistry and clinical aspects of each topic.

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This volume features a comprehensive account of in vitro and in vivo models and in silico approaches for the prediction of oral absorption and bioavailability. It examines the application of virtual screening of virtual libraries as a means of identifying lead molecules for drug discovery programmes. The development of molecular probes targeted to inhibit gamma-secretase, a key enzyme involved in the production of beta-amyloid proteins the accumulation of which has been implicated as a cause of Alzheimer's disease is covered, and progress is reported on the discovery and evaluation of 5-HT terminal autoreceptor antagonists, an approach that may provide a novel treatment of depression. A survey is included of orally acting beta3-agonists for the treatment of type II diabetes and obesity from early compounds active only in rodent models to recent drugs with therapeutic potential in man. Antagonists of the corticotropin releasing factor receptor (CRF) that offer an new approach to the treatment of anxiety and depression, as preliminary clinical data suggests, and possibly of other CNS disorders are also studies, and there is a comprehensive review of inhibitors of phosphodiesterase 5 (PDE5) including compounds that have been advanced into clinical trials.

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This volume includes information on recent advances in five important areas: an account of inhibitors of the caspase family of proteolytic enzymes that represent a new class of anti-inflammatory and antiapoptotic agents of potential value in rheumatoid arthritis; and a survey of semi-synthetic and totally synthetic antibiotics and anti-HIV agents and their sites of interaction; the development of inhibitors of the intracellular enzyme acyl-CoA: cholesterol O-acyltransferase (ACAT) for the treatment of hypercholesterolemia; a description of recent progress in growth hormone secretagogues, with the focus on strategies to improve oral bioavailability and duration of action; and information on inhibition of the proteolytic enzyme, hepatitis C protease N-3(NS3), (required for vital replication) as one of the most attractive targets for HCV infections.

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This volume provides reviews of six topics demonstrating the breadth of the field and recent successes in medicinal chemistry. Each of the first five chapters takes an important biochemical target as its theme and provides an insight into current progress in drug design. The last chapter focuses on the vital subject of pharmacokinetics and the great strides that have been made in this discipline during the past decade. All chapters provide an insight into the skills required of the modern medicinal chemist, in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems. *Presents the latest research in the field of drug discovery *Publishes on a twice yearly basis to bring you the most innovative updates in medicinal chemistry *Available as an online resource via ScienceDirect

「Nielsen BookData」より

Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems. *Presents the latest research in the field of drug discovery *Publishes on a twice yearly basis to bring you the most innovative updates in medicinal chemistry *Available as an online resource via ScienceDirect

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[目次]

  • 1. Finding Protein Kinase Hits Using Structural Information 2. Blunting the Swiss Army Knife 3. Peptide Deformylase Inhibitors 4. Clinically Useful Vanilloid Receptor TRPV1 Antagonists 5. Recent Medicinal Chemistry of the Histamine H3 Receptor 6. Recent Progress in Cannabinoid research 7. Oxytocin Antagonists as Potential Therapeutic Agents

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[目次]

  • Caspase inhibitors as anti-inflammatory and antiapoptotic agents, P.P. Graczyk
  • RNA as a drug target, M.J. Drysdale, et al.
  • ACAT inhibitors - the search for a novel and effective treatment of hypercholesterolemia and atherosclerosis, D.R. Sliskovic, J.A. Picard, B.R. Krause
  • growth hormone secretagogues - discovery of small orally active molecules by peptidomimetic strategies, M. Ankersen
  • inhibitors of hepatitis C virus NS3.4A protease - an overdue line of therapy, R.B. Perni, A.D. Kwong.

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[目次]

  • Pharmacology of Alzheimer's disease, H. Allain et al
  • recent advances in the medicinal chemistry and pharmacology of campothecon, Y. Kawato, H. Terasawa
  • Prodrug design for phosphates and phosphonates, S Freeman, K.C. Ross
  • Aldehydes as biocides, E.G.M. Power
  • Synthetic methods for enantiomers of drugs, R. McCague, G. Casy.

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[目次]

  • Predicting oral absorption and bioavailability, H. van der Waterbeemd, B.C. Jones
  • Virtual screening of virtual libraries, D.V.S. Green
  • Gamma -secretase inhibitors - from molecular probes to new therapeutics, T. Harrison, D. Beher
  • The discovery and development of 5-HT terminal autoreceptor antagonists, J.W. Clitherow et al
  • Orally bioavailable beta3-adrenergic agonists as potential therapeutic agents for obesity and type II diabetes, B. Hu, L.L Jennings
  • Antagonists of the corticotropin releasing factor receptor, J. Saunders, J. Williams
  • Phosphodiesterase type 5, (PDE5) inhibitors, H. Haning, U. Niew hner, E. Bischoff.

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[目次]

  • Preface 1. Human Ether-a-go-go Related Gene (Herg): A Chemist's Perspective 2. Fluorescence Based Assays 3. Selective and Combined Neurokinin Receptor Antagonists 4. Muscarinic Receptor Subtype Pharmacology and Physiology 5. The Transcription Factor NF-eB as Drug Target 6. Recent Advances in the Search for New Antimarial Agents 7. The Discovery of the CCR5 Receptor Antagonist UK-427857. A new agent for the Treatment of HIV infection and AIDS

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[目次]

  • Preface List of Contributors Hit and Lead Identification: Efficient practices for drug discovery DPPIV Inhibition: Promising Therapy for the Treatment of Type 2 Diabetes Recent Progress Towards Nonpeptide Ligands for the Melanocortin-4 Receptor Tuberculosis chemotherapy: recent developments and future perspectives Subject Index Author Index (Volumes 1-45) Subject Index (Volumes 1-45)

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[目次]

  • The discovery and development of atorvastatin, a potent novel hypolipidemic agent, B.D. Roth
  • discovery of CEP-1347/KT-7515, an inhibitor of the JNK/SAPK pathway for the treatment of neurodegenerative diseases, M.S. Saporito, R.L. Hudkins, A.C. Maroney
  • discovery of second generation quinazolinone non-nucleoside reverse transcriptase inhibitors of HIV-1, J.W. Corbett, J.D. Rodgers
  • molecular modeling of opioid receptor-ligand complexes, I. McFadyen, T. Metzger, G. Subramanian, G. Poda, E. Jorvig, D.M. Ferguson.

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[目次]

  • p38 kinase - molecular target for the inhibition of proinflammatory cytokines, J.L. Adams et al
  • the adenosine A3 receptor and its ligands, J.E. Van Muijlwijk-Koezen et al
  • the medicinal chemistry of the P2 receptor family, S.D. Guile et al
  • radioligands for the study of brain 5-HT1A receptors "in vivo", V.W. Pike et al
  • discovery of Montelukast - a once-a-day oral antagonist of leukotriene D4 for the treatment of chronic asthma, R.N. Young
  • the histamine H3 receptor and its ligands, H. Stark et al
  • isothermal titration calorimetry in drug discovery, W.H.J. Ward and G.A. Holdgate.

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[目次]

  • Influenza virus sialidase - a target for drug discovery, M.J. Kiefel and M. Von Itztein
  • fibrinogen receptor antagonists -design and clinical applications, C.D. Eldred and B.J. Judkins
  • combinatorial chemistry as a tool for drug discovery, C.D. Floyd et al
  • new directions in anxiolytic drug research, M.K. Scott et al
  • selective inhibitors of COX-2, J.J. Talley
  • molecularly imprinted polymers - preparation, biomedical applications and technical challenges, C.J. Allender et al.

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この本の情報

書名 Progress in medicinal chemistry
著作者等 Ellis, G. P.
Luscombe, D. K.
Cox Brian
Dax S. L.
Ellis Gwynn P.
King F.D.
Lawton G.
Lawton George
Luscombe D.K. (Welsh School of Pharmacy University of Wales Cardiff Wales)
Oxford A. W.
Reitz A. B.
Witty D. R.
Witty David R.
etc.
West G.B.
巻冊次 v. 1
v. 2
v. 3
v. 4
v. 5
v. 6
v. 7, pt. 1
v. 7, pt. 2
v. 8, pt. 1
v. 8, pt. 2
v. 9, pt. 1
v. 9, pt. 2
v. 10
v. 11
v. 12
v. 13
v. 14
v. 15
v. 16
v. 17
v. 18
v. 19
v. 20
v. 21
v. 22
v. 23
v. 24
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v. 26
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v. 28
v. 29
v. 30
v. 31
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v. 52
v. 53
v. 54
v. 55
v. 56
v. 57
v. 58
v. 59
出版元 Elsevier
刊行年月 [19--]
ページ数 v.
大きさ 22 cm
ISBN 0444500901
0444502947
0444506365
0444509593
0444510540
0444511423
0444511431
0444515720
0444517375
0444528083
0444803459
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0444826327
0444829091
0444894721
0444899898
0720406455
0720406501
0720406552
0720406676
0720406692
0720474000
0720474116
0720474124
0720474108
9780123812902
9780123812926
9780123964939
9780128152133
9780128211731
9780444533005
9780444533586
9780444626523
9780444633804
9780444634801
9780444637154
9780444639394
9780444642776
9780444530189
NCID BA01541473
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言語 英語
出版国 オランダ
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