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.

Chemistry and Molecular Aspects of Drug Design and Action

• Draws from synthetic chemistry, molecular modeling, computational biology, structural genomics, and pharmacology
• Focuses on the correlation of properties and biological activity
• Delves into the phenomenon of xenobiotic metabolism
• Addresses current epidemiological scientific, social, and economic concerns
• Considers the pathobiochemistry of Alzheimer’s, HIV, addiction, environmental and chemical toxicity, as well as cardiovascular, psychological, and neurological diseases

Divided into five parts, each dedicated to various aspects of the classical medicinal chemistry approach, Chemistry and Molecular Aspects of Drug Design and Action makes it easy for readers to focus on a field of specific interest.

1. Chemical, Biochemical, and Biological Aspects of Pathophysiological Conditions
2. Classical Medicinal Chemistry
3. Drug Design, Chemical and Molecular Aspects of Drug Action
4. Drug Xenobiotic Metabolism
5. Physical Organic and Theoretical Medicinal Chemistry

Contents

Chemical, Biochemical, and Biological Aspects of Pathophysiological Conditions

• Inflammatory Mechanisms in Alzheimer’s Disease and other Neurodegenerative Disorders
• Treatment Development Strategies for Alzheimer’s Disease
• Lipoprotein-Associated Phospholipase A2 as a New Prognostic Factor for Coronary Artery Disease
• Protein Modifications by Nitric Oxide and Reactive Nitrogen Species, H. Ischiropoulos

Classical Medicinal Chemistry

• Design, Synthesis, and Pharmacological Evaluation of High Affinity and Selectivity Sigma-1 and Sigma-2 Receptor Ligands
• Synthesis of Biologically Active Taxoids
• From the Molecular Pharmacology to the Medicinal Chemistry of Cannabinoids
• New Inhibitors of DNA Topoisomerase in the Treatment of Experimental Malignancies
• Treatment of Psoriasis with Anthrones – Biochemical Aspects
• An Appraisal of Fomocaines, Current Situation and Outlook
• Ligands for the GABA Recognition Site at the GABAA Receptor: Structure-Activity Studies

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
• A New Class of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI’s) with Great Potential for the Treatment of Human Immunodeficiency Virus Type 1 (HIV-1) Infections
• Histamine H3-Receptor Agonists and Antagonists: Chemical, Pharmacological, and Clinical Aspects
• Anti-Inflammatory Actions of Flavonoids and Structural Requirements
• Molecular Mechanisms of H2O2-Induced DNA Damage: The Action of Desferrioxamine
• LNA (Locked Nucleic Acid) and Functionalized LNA: Towards Efficient Gene Targeting

Drug Xenobiotic Metabolism

• The Effect of Diet on Drug Metabolism
• Cytochromes P450 in the Metabolism and Bioactivation of Chemicals
• In Vitro Methods to Measure Drug Metabolism and Metabolic Interactions in Drug Discovery and Development

Physical Organic and Theoretical Medicinal Chemistry

• How to Probe the Sites of Action of Drug Molecules
• Lipophicility as a Descriptor of Molecular Properties in Drug Design
• Drug Membrane Interaction and the Importance for Drug Transport, Distribution, Accumulation, Efficacy, and Resistance
• Structure-Based and Computer-Aided Drug Design
• Physiochemical Profiling in Early Drug Discovery: New Challenges at the Age of High Throughput Screen and Combinational Chemistry

Index

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