Drug Design

Part I Fundamentalsin Drug Research. - 1. Drug Research Yesterday, Today and Tomorrow. - 2. The Role of Serendipityin Drug Research. - 3. Classical Drug Research. - 4. Protein Ligand Interactionsas the Basis for Drug Action. - 5. Optical Activity and Biological Effects. - Part II Discovery and Optimizationof Lead Compounds. - 6. Screeningfor Lead Structures. - 7. Screening Technologies for LeadDiscovery. - 8. Optimizationof Lead Structures. - 9. Designingprodrugs. - 10. Peptidomimetics. - Part III Experimental and Theoretical Methods. - 11. Combinatorics: Chemistry With Big Numbers. - 12. Gene Technology in drug research. - 13. Experimental Methods of Structure Determination. - 14. The Spatial Structure of Biomolecules. - 15. Molecular Modelling. - 16. Conformational Analysis. - Part IV Structure Activity Relationships and Design Approaches. - 17. Pharmacophore Hypothesis and Molecular Comparisons. - 18. Quantitative Structure ActivityRelationships. - 19. From in vitro to in vivo:Optimization of ADME-Tox Properties. - 20. ProteinModeling and Structure-BasedDrug Design. - 21. ACase Study: Structure-Based Inhibtor Design for tRNA-Guanine Transglycosylase. - Part V. Drugs and drug action: Successes of stucture-based design. - 22. Howdrugs act: Concepts for therapy. - 23. Inhibitors of hydrolases With an acyl-enzymeintermediate. - 24. Asparticprotease inhibitors. - 25. Inhibitorsof hydrolysing metalloenzymes. - 26. Inhibitorsof transferases. - 27. Inhibitors ofoxidoreductases. - 28. Agonists and antagonistsof nuclear receptors. - 29. Agonists and antagonists of membrane-bound. - 30. Ligands forchannels, pores and transporters. - 31. Ligands for surfacereceptors. - 32. Biologicals: Peptides, proteins, nucleotidesand macrolides as drugs.