Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 5

1st Edition - January 28, 1975
Editor: E. J. Ariëns
Language: English
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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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 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