Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 3

1st Edition - January 1, 1972
Editor: E. J. Ariëns
Language: English
eBook ISBN:
9 7 8 - 1 - 4 8 3 2 - 1 6 0 5 - 8

Drug Design, Volume III covers the mode of action of biologically active compounds. The book discusses microbial transformations that have been used in the preparation of drugs… Read more

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Drug Design, Volume III covers the mode of action of biologically active compounds. The book discusses microbial transformations that have been used in the preparation of drugs or closely related substances; the use of linear free energy parameters and other experimental constants in structure-activity studies; and the mode of action of anticoagulants structurally and functionally related to vitamin K. The text also describes the design of beta-blocking drugs, biologically active acridines, local anesthetics, and insect chemosterilants. The molecular approach for designing inhibitors to enzymes involved in blood clotting is also considered. Chemists, pharmacologists, and people involved in drug design.

List of Contributors

Preface

Contents of Other Volumes

Chapter 1. Microbial Conversion as a Tool in the Preparation of Drugs

I. Introduction

II. Practical Aspects of Microbial Transformations

III. Some Theoretical Aspects of Microbial Transformations

IV. Conversions by Microorganisms

References

Chapter 2. The Use of Linear Free Energy Parameters and Other Experimental Constants in Structure-Activity Studies

I. Introduction

II. Parameters Used in Structure-Activity Studies

III. The Multiparameter Approach to Structure-Activity Relationships

IV. Interpretation of Regression Equations

V. Application of the Hansch Approach

References

Chapter 3. Anticoagulants Structurally and Functionally Related to Vitamin K

I. Introduction

II. Mode of Action of Vitamin K

III. Biological Activity of Vitamin K Analogs

IV. The Structure of Compounds with Vitamin K Activity

V. The Structure of Compounds with Anticoagulant Activity

References

Chapter 4. Design of ß-Blocking Drugs

I. Introduction

II. Characteristics of j8-Adrenoceptor Antagonists

III. Structure-Activity Relationships in Arylethanolamines

IV. Other Phenylethanolamine Derivatives

V. Structure-Activity Relationships in Aryloxypropanolamines

VI. Structure-Activity Relationships in Selective j8-Adrenoceptor Antagonists

VII. Other Properties in Relation to j8-Blockade

VIII. Summary

References

Chapter 5. The Design of Biologically Active Acridines

I. Introduction: Ionization and Antibacterial Action

II. Binding to Nucleic Acids: Intercalation and Chemotherapy

III. Prevention of Binding to Nucleic Acids : Pharmacodynamics

IV. Conclusion

References

Chapter 6. The Design of Local Anesthetics

I. Introduction

II. General Considerations on the Development of New Drugs

III. The Classical Procedures for the Development of Local Anesthetics

IV. Rational Methods for the Development of Local Anesthetics

References

Chapter 7. Design of Insect Chemosterilants

I. Introduction

II. Desirable Characteristics of Chemosterilants

III. Methods of Evaluating Chemosterilants

IV. Mechanism of Action

V. Some Unexplored Areas of Research

References

Chapter 8. Molecular Approach for Designing Inhibitors to Enzymes Involved in Blood Clotting

I. Background Information

II. Thrombin

III. Fibrinoligase

IV. Conclusion

References

Author Index

Subject Index