Ariëns Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 6
1. Auflage 2013
ISBN: 978-1-4832-1608-9
Verlag: Elsevier Science & Techn.
Format: PDF
Kopierschutz: 1 - PDF Watermark

E-Book, Englisch, 382 Seiten, Web PDF

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.

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. Diphenhydramine Derivatives: Through Manipulation toward Design;20
8.1;I. Introduction. The Benzhydryl Moiety in Drugs;21
8.2;II. Review of the Synthetic Routes to Structures of the Diphenhydramine Type;22
8.3;II.. The Phase of Manipulation. Classical Approaches to Arrive at Active Structures of the Diphenhydramine Type;43
8.4;IV. Detailed Analysis of the Conditions for Activity in Structures of the Diphenhydramine Type as a Basis for Rational Design;61
8.5;V. Metabolism of Diphenhydramines in Relation to Design;88
8.6;VI. Concluding Remarks;94
8.7;References;95
9;Chapter 2. The Design of Antiradiation Agents;100
9.1;I. Introduction;101
9.2;II. The Nature of Radiation Damage;101
9.3;III. Evaluation of Potential Antiradiation Agents;105
9.4;IV. Theories of Protection;107
9.5;V. Chemical Radioprotective Agents;112
9.6;VI. Other Applications of Antiradiation Drugs;143
9.7;VII. The Future;145
9.8;References;145
10;Chapter 3. Rational Approach to Proteinase Inhibitors;162
10.1;I. Introduction;162
10.2;II. Lysine Homologs as Proteinase Inhibitors;164
10.3;.II. Arginine Homologs as Proteinase Inhibitors;174
10.4;IV. Peptides as Proteinase Inhibitors;182
10.5;V. Coding, Decoding, and Noise in Proteolytic Reactions;185
10.6;References;187
11;Chapter 4. The Design of Organ-Imaging Radiopharmaceuticals;190
11.1;I. Introduction;191
11.2;II. Essential Properties;192
11.3;III. Design Concepts;210
11.4;IV. Imaging Agents—Current Status;214
11.5;References;268
12;Chapter 5. Design of X-Ray Contrast Media;280
12.1;I. The Uses of Radiographic Contrasts Agents (Fig. 2);282
12.2;II. Physical Basics;284
12.3;III. Chemistry of Contrast Agents;286
12.4;IV. Physicochemical Properties of Contrast Agents;294
12.5;V. Toxicology;295
12.6;VI. Pharmacology and Pharmacokinetics;300
12.7;VII. The Risks of X-Ray Contrast Diagnosis;307
12.8;VIII. New Drug Design;307
12.9;References;311
13;Chapter 6. Agricultural Pesticides: Chemical and Physical Methods of Formulation;316
13.1;I. Introduction;317
13.2;II. Pesticides in the Immediate Environment;321
13.3;III. Systemic Pesticides in Agriculture;326
13.4;IV. Physical Formulation;344
13.5;V. Chemical Formulation;359
13.6;References;368
14;Subject Index;372