Drug Design
Medicinal Chemistry: A Series of Monographs, Vol. 5
- 1st Edition - January 28, 1975
- Imprint: Academic Press
- Editor: E. J. Ariëns
- Language: English
- Paperback ISBN:9 7 8 - 1 - 4 8 3 2 - 0 2 6 4 - 8
- eBook ISBN:9 7 8 - 1 - 4 8 3 2 - 1 6 0 7 - 2
Drug Design, Volume V covers the fundamental approaches to the development of bioactive compounds. The book discusses the utilization of operational schemes for analog synthesis in… Read more
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Request a sales quoteDrug Design, Volume V covers the fundamental approaches to the development of bioactive compounds. The book discusses the utilization of operational schemes for analog synthesis in drug design; the design of enzyme inhibitors (transition state analogs); and the significance of structure-absorption-distribution relationships for drug design. The text describes the role of charge-transfer processes in the action of bioactive materials, as well as the approaches to the rational combination of antimetabolites for cancer chemotherapy. The physicochemical, quantum chemical, and other theoretical techniques for the understanding of the mechanism of action of central nervous system (CNS) agents, such as psychoactive drugs, narcotics, and narcotic antagonists and anesthetics, are also encompassed. Chemists, biochemists, pharmacologists, and people involved in drug design will find the book invaluable.
List of Contributors
Preface
Contents of Other Volumes
Chapter 1. Utilization of Operational Schemes for Analog Synthesis in Drug Design
I. Introduction
II. Operational Scheme for Aromatic Substitution
III. Operational Scheme for Side Chains
IV. Examples
V. Rational Follow-up to the Schemes
VI. Conclusion
References
Chapter 2. The Design of Enzyme Inhibitors: Transition State Analogs
I. Introduction
II. Theory of the Transition State Analog Approach
III. Transition State Analogs
IV. Natural Transition State Analog Inhibitors
V. Synthetic Enzymes
VI. Summary
References
Chapter 3. Structure-Absorption-Distribution Relationships: Significance for Drug Design
I. Introduction
II. The Earlier Hypotheses Relating to the Membrane Permeability or Pharmacological Activity with Partition Coefficients
III. Quantitative Correlations Using Multiple Regression Analysis and Substituent Constants
IV. Summary
References
Chapter 4. The Role of Charge-Transfer Processes in the Action of Bioactive Materials
I. Introduction
II. Fundamentals of the Charge-Transfer Process
III. Charge Transfer in Biological Systems
IV. Summary
References
Chapter 5. Approaches to the Rational Combination of Antimetabolites for Cancer Chemotherapy
I. General Introduction
II. Intracellular Metabolic Interactions
III. Alterations in Intracellular Metabolism
IV. Transport or Uptake Interactions
V. Scheduling
VI. Remote Systemic Biotransformation
VII. Modification of Host Nutrients and Toxicity
VIII. Nonmetabolic Combinations
IX. Concluding Remarks
References
Chapter 6. Physicochemical, Quantum Chemical, and Other Theoretical Techniques for the Understanding of the Mechanism of Action of CNS Agents: Psychoactive Drugs, Narcotics, and Narcotic Antagonists and Anesthetics
I. Introduction
II. Evaluation of Quantum Chemical Computational Methods
III. Psychoactive Drugs
IV. Narcotics and Narcotic Antagonists
V. Anesthetics
VI. Recent Developments in Sensitive Methods of Analyses for Normal Neurotransmitters and Their Metabolites
VII. Overall Perspective
References
Subject Index
- Edition: 1
- Published: January 28, 1975
- No. of pages (eBook): 374
- Imprint: Academic Press
- Language: English
- Paperback ISBN: 9781483202648
- eBook ISBN: 9781483216072
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