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. Diphenhydramine Derivatives: Through Manipulation toward Design 20
I. Introduction. The Benzhydryl Moiety in Drugs 21
II. Review of the Synthetic Routes to Structures of the Diphenhydramine Type 22
II.. The Phase of Manipulation. Classical Approaches to Arrive at Active Structures of the Diphenhydramine Type 43
IV. Detailed Analysis of the Conditions for Activity in Structures of the Diphenhydramine Type as a Basis for Rational Design 61
V. Metabolism of Diphenhydramines in Relation to Design 88
VI. Concluding Remarks 94
References 95
Chapter 2. The Design of Antiradiation Agents 100
I. Introduction 101
II. The Nature of Radiation Damage 101
III. Evaluation of Potential Antiradiation Agents 105
IV. Theories of Protection 107
V. Chemical Radioprotective Agents 112
VI. Other Applications of Antiradiation Drugs 143
VII. The Future 145
References 145
Chapter 3. Rational Approach to Proteinase Inhibitors 162
I. Introduction 162
II. Lysine Homologs as Proteinase Inhibitors 164
.II. Arginine Homologs as Proteinase Inhibitors 174
IV. Peptides as Proteinase Inhibitors 182
V. Coding, Decoding, and Noise in Proteolytic Reactions 185
References 187
Chapter 4. The Design of Organ-Imaging Radiopharmaceuticals 190
I. Introduction 191
II. Essential Properties 192
III. Design Concepts 210
IV. Imaging Agents—Current Status 214
References 268
Chapter 5. Design of X-Ray Contrast Media 280
I. The Uses of Radiographic Contrasts Agents (Fig. 2) 282
II. Physical Basics 284
III. Chemistry of Contrast Agents 286
IV. Physicochemical Properties of Contrast Agents 294
V. Toxicology 295
VI. Pharmacology and Pharmacokinetics 300
VII. The Risks of X-Ray Contrast Diagnosis 307
VIII. New Drug Design 307
References 311
Chapter 6. Agricultural Pesticides: Chemical and Physical Methods of Formulation 316
I. Introduction 317
II. Pesticides in the Immediate Environment 321
III. Systemic Pesticides in Agriculture 326
IV. Physical Formulation 344
V. Chemical Formulation 359
References 368
Subject Index 372