Chemistry and Molecular Aspects of Drug Design and Action
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Summary
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.
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.
Table of 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
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