Drug Design - 1st Edition - ISBN: 9780120603060, 9781483216089

Drug Design

1st Edition

Medicinal Chemistry: A Series of Monographs, Vol. 6

Editors: E. J. Ariëns
eBook ISBN: 9781483216089
Imprint: Academic Press
Published Date: 28th January 1975
Page Count: 382
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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.

Table of Contents

List of Contributors


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


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


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


Chapter 4. The Design of Organ-Imaging Radiopharmaceuticals

I. Introduction

II. Essential Properties

HI. Design Concepts

IV. Imaging Agents—Current Status


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


Chapter 6. Agricultural Pesticides: Chemical and Physical Methods of Formulation

I. Introduction

II. Pesticides in the Immediate Environment

III. Systemic Pesticides in Agriculture

IV. Physical Formulation

V. Chemical Formulation


Subject Index


No. of pages:
© Academic Press 1975
Academic Press
eBook ISBN:

About the Editor

E. J. Ariëns

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