Drug Design
Medicinal Chemistry: A Series of Monographs, Vol. 3
- 1st Edition - January 1, 1972
- Imprint: Academic Press
- Editor: E. J. Ariëns
- Language: English
- Paperback ISBN:9 7 8 - 1 - 4 8 3 2 - 0 2 6 2 - 4
- 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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Request a sales quoteDrug 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
- Edition: 1
- Published: January 1, 1972
- No. of pages (eBook): 520
- Imprint: Academic Press
- Language: English
- Paperback ISBN: 9781483202624
- eBook ISBN: 9781483216058
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