Drug Design

Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 5

1st Edition - January 28, 1975

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  • Editor: E. J. Ariëns
  • eBook ISBN: 9781483216072

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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.

Table of Contents

  • List of Contributors


    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


    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


    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


    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


    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


    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


    Subject Index

Product details

  • No. of pages: 374
  • Language: English
  • Copyright: © Academic Press 1975
  • Published: January 28, 1975
  • Imprint: Academic Press
  • eBook ISBN: 9781483216072

About the Editor

E. J. Ariëns

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