Ariëns Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 3
1. Auflage 2013
ISBN: 978-1-4832-1605-8
Verlag: Elsevier Science & Techn.
Format: PDF
Kopierschutz: 1 - PDF Watermark

E-Book, Englisch, 520 Seiten, Web PDF

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.

Autoren/Hrsg.

Ariëns, E. J.

Inhaltsverzeichnis

1;Front Cover;1
2;Drug Design;4
3;Copyright Page;5
4;Table of Contents;6
5;List of Contributors;10
6;Preface;12
7;Contents of Other Volumes;14
8;Chapter 1. Microbial Conversion as a Tool in the Preparationof Drugs;20
8.1;I. Introduction;22
8.2;II. Practical Aspects of Microbial Transformations;24
8.3;III. Some Theoretical Aspects of Microbial Transformations;31
8.4;IV. Conversions by Microorganisms;53
8.5;ACKNOWLEDGMENTS;136
8.6;REFERENCES;136
9;Chapter 2. The Use of Linear Free Energy Parameters and Other Experimental Constants in Structure–Activity Studies;152
9.1;I. Introduction;152
9.2;II. Parameters Used in Structure-Activity Studies;158
9.3;III. The Multiparameter Approach to Structure-Activity Relationships;179
9.4;IV. Interpretation of Regression Equations;186
9.5;V. Application of the Hansch Approach;194
9.6;ACKNOWLEDGMENTS;201
9.7;REFERENCES;201
10;Chapter 3. Anticoagulants Structurally and Functionally Related to Vitamin K;208
10.1;I. Introduction;208
10.2;II. Mode of Action of Vitamin K;210
10.3;III. Biological Activity of Vitamin K Analogs;211
10.4;IV. The Structure of Compounds with Vitamin K Activity;212
10.5;V. The Structure of Compounds with Anticoagulant Activity;217
10.6;REFERENCES;220
11;Chapter 4. Design of ß-Blocking Drugs;224
11.1;I. Introduction;224
11.2;II. Characteristics of ß-Adrenoceptor Antagonists;230
11.3;III. Structure-Activity Relationships in Arylethanolamines;232
11.4;IV. Other Phenylethanolamine Derivatives;234
11.5;V. Structure-Activity Relationships in Aryloxypropanolamines;235
11.6;VI. Structure-Activity Relationships in Selective ß-Adrenoceptor Antagonists;238
11.7;VII. Other Properties in Relation to ß-Blockade;241
11.8;VIII. Summary;245
11.9;REFERENCES;245
12;Chapter 5. The Design of Biologically Active Acridines;248
12.1;I. Introduction: Ionization and Antibacterial Action;248
12.2;II. Binding to Nucleic Acids: Intercalation and Chemotherapy;250
12.3;III. Prevention of Binding to Nucleic Acids : Pharmacodynamics;259
12.4;IV. Conclusion;260
12.5;REFERENCES;260
13;Chapter 6. The Design of Local Anesthetics;262
13.1;I. Introduction;263
13.2;II. General Considerations on the Development of New Drugs;264
13.3;III. The Classical Procedures for the Development of Local Anesthetics;265
13.4;IV. Rational Methods for the Development of Local Anesthetics;325
13.5;References;400
14;Chapter 7. Design of Insect Chemosterilants;412
14.1;I. Introduction;412
14.2;II. Desirable Characteristics of Chemosterilants;414
14.3;III. Methods of Evaluating Chemosterilants;415
14.4;IV. Mechanism of Action;417
14.5;V. Some Unexplored Areas of Research;430
14.6;REFERENCES;431
15;Chapter 8. Molecular Approach for Designing Inhibitors to Enzymes Involved in Blood Clotting;434
15.1;I. Background Information;434
15.2;II. Thrombin;438
15.3;III. Fibrinoligase;450
15.4;IV. Conclusion;462
15.5;REFERENCES;464
16;Author Index;468
17;Subject Index;494