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Chemistry and Molecular Aspects of Drug Design and Action

Edited by E. A. Rekka, P. N. Kourounakis

Contributors: Yvette Tache, Costas Ioannides, Olavi Pelkonen, Rolf W. Hartmann, Holger Stark, Alexandros Makriyannis, Erik De Clercq, Joseph Rogers, Alexandros D. Tselepis, Jacques H. Poupaert, K.C. Nicolaou, Didier M. Lambert, Wolfgang Wiegrebe, Herbert Oelschlager, Bente Frolund, Theoharis C. Theoharides, Dimitrios Galaris, Jesper Wengel, Karl Joachim Netter, Hugo Kubinyi, Bernard Faller, Ernst Wulfert, L. Holzgrabe, Povl Krogsgaard-Larsen, Tommy Liljefors, Walter Schunack, Rena Li, Zhe Liang, Lih-Fen Lue, Alexander Roher, Marwan Sabbagh, Yong Shen, Ronald Strohmeyer, Douglas Walker, R.K. Guy, Klaus Muller, Uffe Kristiansen, U. Muller-Vieira, Sarah Ulmschneider, M. Voets, A. Karlsson, Jan Balzarini, P.T. Doulias, Margarita Tenopoulou, M. Turpeinen, J. Uusitalo, Paivi Taavitsainen, Hannu Raunio, Francis Bitter, A.P. Kourounakis

Published April 28th 2008 by CRC Press – 384 pages

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Description

An ever-increasing demand for better drugs, elevated safety standards, and economic considerations have all led to a dramatic paradigm shift in the way that drugs are being discovered and developed. Known as rational drug design, this contemporary process is defined by three main steps: the discovery of lead compounds, surgical manipulation to develop pharmacophores, and further optimization to produce the best compounds.

Chemistry and Molecular Aspects of Drug Design and Action brings together an impressive collection of world-renowned pharmacochemistry scientists who are currently defining the emergence of rational drug design. Offering insight from their own specialized research, these pioneers highlight the variety of approaches being employed in this field, including those that start by considering either molecular mechanisms of drug action, or the metabolizing enzyme action occurring in the structure of a drug molecule. Another approach they explore is one that starts from the pathobiochemistry and pathophysiology of target diseases. Furthermore, the book also considers drug development that makes use of already developed compounds stored in data banks.

Divided into five parts, each dedicated to various aspects of the classical medicinal chemistry approach, the text makes it easy for readers to focus on a field of specific interest.

  • Chemical, Biochemical, and Biological Aspects of Pathophysiological Conditions
  • Classical Medicinal Chemistry
  • Drug Design, Chemical and Molecular Aspects of Drug Action
  • Drug Xenobiotic Metabolism
  • Physical Organic and Theoretical Medicinal Chemistry

    • While each section can be studied independently, the combined material in this volume provides the most comprehensive overview available on rational drug design. This work is an invaluable resource both for those entering the field, as well as those researchers looking to build on current progress.

    Contents

    Introduction: Rational Drug Design Based Mainly on the Pathobiochemistry of the Disease, E.A. Rekka, A.P. Kourounakis, and P.N. Kourounakis

     

    Part I: Chemical, Biochemical, and Biological

    Aspects of Pathophysiological Conditions

    Inflammatory Mechanisms in Alzheimer’s Disease and Other

    Neurodegenerative Disorders, J. Rogers, T. Beach, R. Li, Z. Liang,

    L.-F. Lue, A. Roher, M. Sabbagh, Y. Shen, R. Strohmeyer, and D. Walker

    Treatment Development Strategies for Alzheimer’s Disease, E. Wülfert

    Lipoprotein-Associated Phospholipase A2 as a New Prognostic

    Factor for Coronary Artery Disease, A.D. Tselepis

    New Molecular Targets for the Prevention and Treatment of

    Gastrointestinal Ulcers and Inflammation

    S. Szabo, G. Tolstanova, L. Nagy, L. Chen, T. Khomenko, X. Deng, and Z. Sandor

    Stress Activates Corticotropin Releasing: Factor Signaling

    Pathways: Implication in Functional Bowel Disorders, Y. Taché

    Part II

    Classical Medicinal Chemistry

    Design, Synthesis, and Pharmacological Evaluation of

    High-Affinity and Selectivity Sigma-1 and Sigma-2 Receptor

    Ligands, J.H. Poupaert

    Synthesis of Biologically Active Taxoids, K.C. Nicolaou and R.K. Guy

    From the Molecular Pharmacology to the Medicinal Chemistry

    of Cannabinoids, D.M. Lambert

    An Appraisal of Fomocaines: Current Situation and Outlook,

    H. Oelschläger and A. Seeling

    Ligands for the GABA Recognition Site at the GABAA

    Receptor: Structure-Activity Studies, B. Frølund, U. Kristiansen, P. Krogsgaard-Larsen, and T. Liljefors

    Strategies for Development of New Lead Structures for

    Inhibition of Acetylcholinesterase, P. Kapkova, V. Alptuzun, E. Heller,

    E. Kugelmann, G. Folkers, and U. Holzgrabe

    Part III

    Drug Design, Chemical and Molecular

    Aspects of Drug Action

    Discovery of Potent and Selective Inhibitors of Human

    Aldosterone Synthase (CYP11B2): A New Target for the

    Treatment of Congestive Heart Failure and Myocardial

    Fibrosis—a Review, R.W. Hartmann, U. Müller-Vieira, S. Ulmschneider, and M. Voets

    Thiocarboxanilides: A New Class of Nonnucleoside Reverse

    Transcriptase Inhibitors (NNRTIs) with Great Potential for the

    Treatment of Human Immunodeficiency Virus Type 1 (HIV-l)

    Infections, E. De Clercq, A. Karlsson, and J. Balzarini

    Histamine H3-Receptor Agonists and Antagonists: Chemical,

    Pharmacological, and Clinical Aspects, H. Stark and W. Schunack

    Anti-Inflammatory Actions of Flavonoids and Structural

    Requirements for New Design, T.C. Theoharides

    Molecular Mechanisms of H2O2-Induced DNA Damage: The Action of Desferrioxamine, M. Tenopoulou, P.-T. Doulias, and D. Galaris

    LNA (Locked Nucleic Acid) and Functionalized LNA: Toward Efficient Gene Targeting, J. Wengel

    Part IV

    Drug – Xenobiotic Metabolism

    The Effect of Diet on Drug Metabolism, K.J. Netter

    Cytochromes P450 in the Metabolism and Bioactivation of

    Chemicals, C. Ioannides

    In Vitro Methods to Measure Drug Metabolism and Drug

    Interactions in Drug Discovery and Development, O. Pelkonen, M. Turpeinen, J. Uusitalo, P. Taavitsainen, and H. Raunio

    Part V

    Physical Organic and Theoretical

    Medicinal Chemistry

    How to Probe the Sites of Action of Drug Molecules, A. Makriyannis and F. Bitter

    Physicochemical Profiling in Early Drug Discovery: New Challenges at the Age of High-Throughput Screen and Combinatorial Chemistry, B. Faller

    Drug-Membrane Interaction and Its Importance for Drug

    Efficacy, J.K. Seydel, E.A. Coats, K. Visser, and M. Wiese

    The Fight Against AIDS: New Avenues for Inhibiting Reverse

    Transcriptase (RT), an Old Target, M. Botta, L. Angeli, M. Radi, and G. Maga

    Name: Chemistry and Molecular Aspects of Drug Design and Action (Hardback) – CRC Press 
    Description: Edited by E. A. Rekka, P. N. KourounakisContributors: Yvette Tache, Costas Ioannides, Olavi Pelkonen, Rolf W. Hartmann, Holger Stark, Alexandros Makriyannis, Erik De Clercq, Joseph Rogers, Alexandros D. Tselepis, Jacques H. Poupaert, K.C. Nicolaou, Didier M. Lambert, Wolfgang Wiegrebe, Herbert Oelschlager, Bente Frolund, Theoharis C. Theoharides, Dimitrios Galaris, Jesper Wengel, Karl Joachim Netter, Hugo Kubinyi, Bernard Faller, Ernst Wulfert, L. Holzgrabe, Povl Krogsgaard-Larsen, Tommy Liljefors, Walter Schunack, Rena Li, Zhe Liang, Lih-Fen Lue, Alexander Roher, Marwan Sabbagh, Yong Shen, Ronald Strohmeyer, Douglas Walker, R.K. Guy, Klaus Muller, Uffe Kristiansen, U. Muller-Vieira, Sarah Ulmschneider, M. Voets, A. Karlsson, Jan Balzarini, P.T. Doulias, Margarita Tenopoulou, M. Turpeinen, J. Uusitalo, Paivi Taavitsainen, Hannu Raunio, Francis Bitter, A.P. Kourounakis. An ever-increasing demand for better drugs, elevated safety standards, and economic considerations have all led to a dramatic paradigm shift in the way that drugs are being discovered and developed. Known as rational drug design, this contemporary...
    Categories: Medicinal & Pharmaceutical Chemistry, Pharmaceutical Science, Pharmacology