Drug Stereochemistry

Professor Krzysztof Jóźwiak is head of laboratory of medicinal chemistry and neuroengineering of Medical University of Lublin, Poland Dr W John Lough is reader in pharmaceutical analysis in the Department of Pharmacy, Health and Well-Being at the University of Sunderland, UK Irving W. Wainer, Ph.D. is senior investigator, in the Bioanalytical Chemistry and Drug Discovery Section, Laboratory for Clinical Investigation, National Institute of Aging/National Institutes of Health

Introduction: The Early History of Stereochemistry: From the Discovery of Molecular Asymmetry and the First Resolution of a Racemate by Pasteur to the Asymmetrical Chiral Carbon of Van’t Hoff and Le Bel. Stereochemical Terms and Concepts: An Overview. Molecular Chiral Recognition: An Introduction and Overview. The Role of Stereo-Chemistry in the Development of ACE Inhibitors: Nature to Clinic. The Separation, Preparation and Identification of Stereochemically Pure Drugs: Indirect Methods for the Chromatographic Resolution of Drug Enantiomers: Synthesis and Separation of Diastereo-Metric Derivatives. The Direct Resolution of Enantiometric Drugs by Chiral Phase Gas Chromatography. HPLC Chiral Stationary Phases for the Stereochemical Resolution of Enantiometric Compounds: The Current State of the Art. Enantioselective Separations by Capillary Electrophoresis. Recent Advances in the Synthesis of Enantiomerically Pure Compounds. Production Scale Preparation of Enantiomerically Pure Compounds by Chromatography and Synthetic Approaches. Spectrometric Identification and Characterization of Chiral Molecules. Pharmacokinetic and Pharmacodynamic Differences Between Drug Stereoisomers: Stereochemical Considerations in the ADMET Stage of Drug Development. Stereoselective Biotransformations: Toxico-Logical Consequences and Implications. Stereoselective Interactions with Enzymes and Their Use in Drug Development. Stereoselective Transport of Drugs Across Epithelia. Clinical Pharmacokinetics and pharmacodynamics of Stereoisomeric Drugs. Industrial and Regulatory Perspectives on Single Isomer Drugs: Regulatory Perspective of the Development of New Stereoisomeric Drugs. Stereochemically Pure Drugs Versus Racemates: An Overview. The Development and Marketing of Single Isomer Drugs vs Racemates: A Legal Perspective.