Drug Design

List of Contributors

Preface

Contents of Other Volumes

Chapter 1. Advances in the Methodology of Quantitative Drug Design

I. How Should the Original Lead Be Used in the Design of Analogs?

II. Which Physical Properties Should Be Related to Potency?

III. Calculation, Measurement, and Meaning of Partition Coefficients

IV. Theoretical Compartment Models for the Relationship between Physical Properties and Biological Potency

V. Mathematical Methods for the Analysis of QSAR

VI. Overview

References

Chapter 2. The Application of Pattern Recognition to Drug Design

I. Introduction

II. Pattern Recognition: Philosophy and Methodology

III. Pattern Recognition Applications

IV. Conclusions

References

Chapter 3. The Design of Controlled Drug Delivery Systems

I. Introduction

II. Therapeutic Systems for Controlled Drug Delivery

III. Two Therapeutic Systems for Clinical Use

IV. The ALZET® Osmotic Minipump for Animal Studies

V. Conclusions

References

Chapter 4. Receptor Binding as a Tool in the Development of New Bioactive Steroids

I. Introduction

II. Characterization of Steroid Hormone Receptors

III. Screening Methodology

IV. Screening Results

V. Conformation Studies

VI. Correlation between Binding Affinity and Biological Potency

VII. Conclusion

References

Chapter 5. The Design of Synthetic Sweeteners

I. Introduction

II. Design Concepts

III. Current and Future Trends

References

Chapter 6. The Prospective Assessment of Environmental Effects of Chemicals

I. Introduction

II. Identification of the Problem

III. Types of Tests To Be Carried Out

IV. Choice of Test Organisms

V. Setup of the Test Program

VI. Areas for Further Research

VII. Conclusions

References

Chapter 7. Design of Selective Ion Binding Macrocyclic Compounds and Their Biological Applications

I. Introduction

II. Historical Perspective

III. Nomenclature and Physical Properties

IV. Biological Applications

V. Synthesis

VI. Organic Reactions

VII. Structural Relationships

VIII. Cation Selectivities

IX. Potential of Macrocyclic Compounds as Drugs

References

Index