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Medicinal Chemistry for the 21st Century
A "Chemistry for the 21st Century Monograph".

C.G. Wermuth, N. Koga, H. Koning, and B.M. Metcalf, eds.

Blackwell Science, 1992 [ISBN 0-632-03408-4]

A timely volume devoted to articles on the design and development of new chemical molecules for the treatment, cure or prevention of human and animal diseases. It is recognized that three critical stages govern the development of new drugs: the improvement of the compound in terms of potency, selectivity and safety; and the adaptation of the molecules to its clinical use. This book looks in detail at theses three stages concentrating on the quest for new lead discovery in Part 1. Protein structure - function relationships are outlined in Part 2, which deals with cloning and structural studies on receptors and enzymes, detection of new enzymes and receptors by hybridization techniques, and signal transduction and mechanisms. Knowledge of protein structure and mechanism of signal transduction are an absolute requisite for medicinal chemists dealing with drug design. Part 3 covers structure - activity relationships dealing with pharmacophore mimickry modelling, design and peptidomimetics, and optimization. Finally, Part 4 is devoted to chemical formulation and to specific administration devices in order to ascertain optimal bioavailability of the active molecules and to render them chemically efficient.

Contents

Past Approaches to Discovering New Drugs; Reflections and Perspectives; Trends In New Lead Identification: A Structural Approach; From Membrane to Genomic Pharmacology or from Short-Term to Long-Term Effects; Future Applications of Oligonucleotides in Antiviral and Antitumoral Chemotherapy; Molecular Biology of Drug Receptors and the Advent of Reverse Pharmacoly; A Structural Basis for Proteinase-Protein Inhibitor Interaction; New Approaches to Isolation, Expression and Molecular Modelling of Proteases; New Era of Biochemistry: Cytokine Signal Network and its Implication for Biomedical Research; Molecular Mechanisms of Regulatory Signal Transduction; Molecular Diversity of Signal Transduction Systems: A Puzzle for Pharmacologists of Today and Tomorrow; The Future of Computer-Aided Drug Design; Pharmacophore Identification Based on Molecular Electrostatic Potentials (MEPS); New Rational Approaches for Structure-Activity Relationships and Drugs Design; Rational Design of Peptidomimetics: Structural and Pharmacological Aspects; Non-Peptide Ligands for Peptide Receptors; Peptidometic Research, Design and Synthesis; Peptidomimetics as Tools for the Initiation and Analysis of Peptide and Protein Secondary Structure: the Prospects for Unnatural Proteins by Design; On the Future QSAR; Computer-Assisted Drug Design in the 21st Century; Trends in Design of Prodrugs for Improved Drug Delivery; Antibody-Based Drug Targeting Approaches: Perspectives and Challenges; Novel Drug-Delivery Systems; Lipid Microsphere Preparations and Lecithinized Peptides For Drug-Delivery Systems.

 


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