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Drug Design
Medicinal Chemistry: A Series of Monographs, Vol. 6
1st Edition - January 28, 1975
Editor: E. J. Ariëns
Language: English
eBook ISBN:9781483216089
9 7 8 - 1 - 4 8 3 2 - 1 6 0 8 - 9
Drug Design, Volume VI covers practical approaches to the development of bioactive compounds, with focus on antiradiation agents, organ-imaging radiopharmaceuticals, X-ray contrast…Read more
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Drug Design, Volume VI covers practical approaches to the development of bioactive compounds, with focus on antiradiation agents, organ-imaging radiopharmaceuticals, X-ray contrast media, proteinase inhibitors, and pesticide formulations. The book discusses the chemical routes available for the synthesis of diphenhydramine derivatives, the biological activities, the relationships between structure and activity, and the phase of manipulation in the design of diphenhydramine derivatives. The text also describes the design of antiradiation agents, organ-imaging radiopharmaceuticals, and X-ray contrast media, as well as the rational approach to proteinase inhibitors. The chemical and physical methods of formulation of agricultural pesticides are also encompassed. Chemists, biochemists, pharmacologists, and people involved in drug design and manufacture will find the book invaluable.
List of Contributors
Preface
Contents of Other Volumes
Chapter 1. Diphenhydramine Derivatives: Through Manipulation toward Design
I. Introduction. The Benzhydryl Moiety in Drugs
II. Review of the Synthetic Routes to Structures of the Diphenhydramine Type
III. The Phase of Manipulation. Classical Approaches to Arrive at Active Structures of the Diphenhydramine Type
IV. Detailed Analysis of the Conditions for Activity in Structures of the Diphenhydramine Type as a Basis for Rational Design
V. Metabolism of Diphenhydramines in Relation to Design
VI. Concluding Remarks
References
Chapter 2. The Design of Antiradiation Agents
I. Introduction
II. The Nature of Radiation Damage
III. Evaluation of Potential Antiradiation Agents
IV. Theories of Protection
V. Chemical Radioprotective Agents
VI. Other Applications of Antiradiation Drugs
VII. The Future
References
Chapter 3. Rational Approach to Proteinase Inhibitors
I. Introduction
II. Lysine Homologs as Proteinase Inhibitors
III. Arginine Homologs as Proteinase Inhibitors
IV. Peptides as Proteinase Inhibitors
V. Coding, Decoding, and Noise in Proteolytic Reactions
References
Chapter 4. The Design of Organ-Imaging Radiopharmaceuticals
I. Introduction
II. Essential Properties
HI. Design Concepts
IV. Imaging Agents—Current Status
References
Chapter 5. Design of X-Ray Contrast Media
I. The Uses of Radiographic Contrast Agents
II. Physical Basics
III. Chemistry of Contrast Agents
IV. Physicochemical Properties of Contrast Agents
V. Toxicology
VI. Pharmacology and Pharmacokinetics
VII. The Risks of X-Ray Contrast Diagnosis
VIII. New Drug Design
References
Chapter 6. Agricultural Pesticides: Chemical and Physical Methods of Formulation