Drug Design (eBook)

Front Cover 1
Drug Design 4
Copyright Page 5
Table of Contents 6
List of Contributors 10
Preface 12
Contents of Other Volumes 14
Chapter 1. Microbial Conversion as a Tool in the Preparationof Drugs 20
I. Introduction 22
II. Practical Aspects of Microbial Transformations 24
III. Some Theoretical Aspects of Microbial Transformations 31
IV. Conversions by Microorganisms 53
ACKNOWLEDGMENTS 136
REFERENCES 136
Chapter 2. The Use of Linear Free Energy Parameters and Other Experimental Constants in Structure–Activity Studies 152
I. Introduction 152
II. Parameters Used in Structure-Activity Studies 158
III. The Multiparameter Approach to Structure-Activity Relationships 179
IV. Interpretation of Regression Equations 186
V. Application of the Hansch Approach 194
ACKNOWLEDGMENTS 201
REFERENCES 201
Chapter 3. Anticoagulants Structurally and Functionally Related to Vitamin K 208
I. Introduction 208
II. Mode of Action of Vitamin K 210
III. Biological Activity of Vitamin K Analogs 211
IV. The Structure of Compounds with Vitamin K Activity 212
V. The Structure of Compounds with Anticoagulant Activity 217
REFERENCES 220
Chapter 4. Design of ß-Blocking Drugs 224
I. Introduction 224
II. Characteristics of ß-Adrenoceptor Antagonists 230
III. Structure-Activity Relationships in Arylethanolamines 232
IV. Other Phenylethanolamine Derivatives 234
V. Structure-Activity Relationships in Aryloxypropanolamines 235
VI. Structure-Activity Relationships in Selective ß-Adrenoceptor Antagonists 238
VII. Other Properties in Relation to ß-Blockade 241
VIII. Summary 245
REFERENCES 245
Chapter 5. The Design of Biologically Active Acridines 248
I. Introduction: Ionization and Antibacterial Action 248
II. Binding to Nucleic Acids: Intercalation and Chemotherapy 250
III. Prevention of Binding to Nucleic Acids : Pharmacodynamics 259
IV. Conclusion 260
REFERENCES 260
Chapter 6. The Design of Local Anesthetics 262
I. Introduction 263
II. General Considerations on the Development of New Drugs 264
III. The Classical Procedures for the Development of Local Anesthetics 265
IV. Rational Methods for the Development of Local Anesthetics 325
References 400
Chapter 7. Design of Insect Chemosterilants 412
I. Introduction 412
II. Desirable Characteristics of Chemosterilants 414
III. Methods of Evaluating Chemosterilants 415
IV. Mechanism of Action 417
V. Some Unexplored Areas of Research 430
REFERENCES 431
Chapter 8. Molecular Approach for Designing Inhibitors to Enzymes Involved in Blood Clotting 434
I. Background Information 434
II. Thrombin 438
III. Fibrinoligase 450
IV. Conclusion 462
REFERENCES 464
Author Index 468
Subject Index 494