Smith and Williams' Introduction to the Principles of Drug Design and Action
Höfundar:
H. John Smith; Hywel Williams (Útgáfa: 4)
Kaup valmöguleikar
Nánar um bókina
- Taylor & Francis
- 9781135299750
- 9781032306612
- ePub
- 4
- H. John Smith; Hywel Williams
- English
- 2005-10-10
- 100
- 2
- 2
Kaflar
- Cover Page
- Title Page
- Copyright Page
- Preface
- List of Contributors
- Abbreviations
- 1. Processes of Drug Handling by the Body
- 1.1 Introduction
- 1.2 Absorption
- 1.3 Distribution
- 1.4 Metabolism
- 1.5 Removal of Drugs from the Body
- 1.6 Summary
- Further Reading
- 2. The Design of Drug Delivery Systems
- 2.1 Introduction
- 2.2 Formulation Aims
- 2.3 Physico-Chemical Factors Influencing Drug Bioavailability
- 2.4 Influence of Route of Administration and Type of Dosage Form
- 2.5 Formulation Factors
- 2.6 Drug Delivery to the Lung
- 2.7 Sustained and Controlled Release Dosage Forms
- 2.8 Site-Specific Drug Delivery
- 2.9 Bioequivalence
- Further Reading
- 3. Intermolecular Forces and Molecular Modelling
- 3.1 Introduction
- 3.2 Molecular Interactions
- 3.3 Free Energies of Interaction—Gas phase and Solution
- 3.4 Intramolecular Forces and Conformation
- 3.5 Molecular Modelling
- 3.6 Proteins
- 3.7 Accurate Calculation of Intermolecular Interactions
- References
- 4. Drug Chirality and Its Pharmacological Consequences
- 4.1 Introduction
- 4.2 Definitions and Nomenclature
- 4.3 Biological Activity
- 4.4 Pharmacokinetic Considerations
- 4.5 Pharmacodynamic Considerations
- 4.6 Selected Therapeutic Groups
- 4.7 Toxicology
- 4.8 Racemates Versus Enantiomers: The Future
- 4.9 Concluding Comment
- Further Reading
- 5. Quantitative Structure-Activity Relationships and Drug Design
- 5.1 Introduction
- 5.2 Hydrophobicity Parameters
- 5.3 Electronic Parameters
- 5.4 Steric Parameters
- 5.5 Topological Parameters
- 5.6 Biological Relationships
- 5.7 Some Limitations and Pitfalls of QSAR
- 5.8 Multivariate Analysis
- 5.9 Neural Networks
- 5.10 Summary
- Further Reading
- 6. From Programme Sanction to Clinical Trials: A Partial View of the Quest for Arimidex™, A Potent, Selective Inhibitor of Aromatase
- 6.1 Introduction
- 6.2 Background
- 6.3 ICI Start on Aromatase Inhibition
- 6.4 Aromatase Resumed
- 6.5 Bis-Triazole (6.17)—A Timely Aromatase Compound in Development
- 6.6 The Search for the Ideal Back-Up Candidate
- 6.7 Into the Clinic
- Further Reading
- 7. Pro-Drugs
- 7.1 Introduction
- 7.2 Pro-Drug Design
- 7.3 Application to Pharmaceutical Problems
- 7.4 Pharmacological Problems
- 7.5 Summary
- Further Reading
- 8. Design of Enzyme Inhibitors as Drugs
- 8.1 Introduction
- 8.2 General Aspects of Inhibitor Design
- 8.3 Rational Approach to the Design of Enzyme Inhibitors
- 8.4 Development of a Successful Drug for the Clinic
- 8.5 Stereoselectivity
- 8.6 Examples of Enzyme Inhibitors as Drugs
- Further Reading
- 9. The Chemotherapy of Cancer
- 9.1 Introduction
- 9.2 Terminology
- 9.3 Metastases
- 9.4 Cell Growth Cycle
- 9.5 Mechanisms of Tumour Formation
- 9.6 Treatment
- 9.7 Antimetabolites
- 9.8 DNA Interactive Compounds
- 9.9 Antitubulin Agents
- 9.10 Miscellaneous Agents
- 9.11 Immunosuppressive Agents
- 9.12 Anti-Hormonal Agents
- 9.13 Enzymes
- 9.14 Biologicals
- 9.15 Prodrugs and Drug Targeting Approaches
- 9.16 New Research Tools
- 9.17 Future Possibilities
- 9.18 Anti-Emetics
- Further Reading
- 10. Neurotransmitters, Agonists and Antagonists
- 10.1 Overview
- Further Reading
- 10.2 Serotonin Receptors and Ligands
- Further Reading
- 10.3 Histamine Receptors
- Further Reading
- 10.4 Dopamine Receptors
- Further Reading
- 11. Design of Antimicrobial Chemotherapeutic Agents
- 11.1 Introduction
- 11.2 Production of Chemotherapeutic Agents
- 11.3 Mechanism of Action of Chemotherapeutic Agents
- 11.4 Bacterial Resistance to Chemotherapeutic Agents
- 11.5 Design of β-Lactam Antibiotics
- 11.6 Design of Other Antibacterial Agents
- 11.7 Design of Antifungal Agents
- 11.8 Design of Antiviral Agents
- 11.9 Overall Conclusions and Comments
- Further Reading
- 12. Recombinant DNA Technology: Monoclonal Antibodies
- 12.1 Recombinant DNA Technology
- 12.2 Monoclonal Antibodies
- Further Reading
- 13. Bio-Inorganic Chemistry and Its PharmaceuticaL Applications
- 13.1 Introduction
- 13.2 The Importance of Trace Elements in Humans
- 13.3 Metal Coordination Chemistry
- 13.4 PHarmacological and Pharmaceutical Considerations
- 13.5 Metals as the Modus Operandi of Drugs
- 13.6 Drugs which Exert Their Effects Via Metal Complexation or Chelation
- 13.7 Metal-Dependent Side Effects of Drugs
- 13.8 Trace Element Supplementation
- 13.9 Concluding Remarks
- Further Reading