Ariëns Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 10
1. Auflage 2013
ISBN: 978-1-4832-1611-9
Verlag: Elsevier Science & Techn.
Format: PDF
Kopierschutz: 1 - PDF Watermark

E-Book, Englisch, 446 Seiten, Web PDF

Drug Design, Volume X covers promising and current developments in drug design. The book discusses procedures as applied in the practice of drug design; the structural aspects of the structure-activity relationships of neuroleptics; and promising perspectives in the highly actual field of bioactive peptides. The text also describes the application of the dynamic systems analysis to the antihypertensive drug action; polymeric drug delivery systems; and the design of biocompatible polymers. The structure-activity relationships of insect repellents as a basis for the design of such agents, as well as the approaches to the multivariate data analysis in structure-activity relationships, which is an essential aspect of drug design, are also encompassed. Chemists, pharmacologists, bioengineers, 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;Chapter 1. Practical Procedures in Drug Design;14
7.1;I. Introduction;14
7.2;II. General Aspects of Drug Development;15
7.3;III. Procedures in Drug Design;17
7.4;IV. Application of the Theory of Sets to Drug Design;20
7.5;V. Drug Design in Practice;30
7.6;VI. Conclusion;80
7.7;References;80
8;Chapter 2. Structural Aspects of the Structure-Activity Relationships of Neuroleptics: Principles and Methods;84
8.1;I. Introduction;85
8.2;II. Conformational Analysis;86
8.3;III. Determination of Molecular Structure;90
8.4;IV. Description and Comparison of Molecular Structures;110
8.5;V. Summary and Conclusions;127
8.6;ACKNOWLEDGMENTS;128
8.7;References;128
9;Chapter 3. Bridging the Gap between Bioactive Peptides and Nonpeptides: Some Perspectives in Design;132
9.1;I. Introduction;132
9.2;II. Design of Nonpeptidic Peptidomimetics;139
9.3;III. Conclusions;154
9.4;ACKNOWLEDGMENTS;154
9.5;References;154
10;Chapter 4. Dynamic Systems Analysis as a Basis for Drug Design: Application to Antihypertensive Drug Action;158
10.1;I. Introduction;159
10.2;II. Dynamics of Drug Action;161
10.3;III. Antihypertensive Drugs: Dynamics of the Interactions with the Cardiovascular System;170
10.4;IV. Pharmacotherapy of Hypertensive Disease;194
10.5;V. Dynamic Systems Analysis as a Basis for Drug Design;197
10.6;References;199
11;Chapter 5. Polymeric Drug Delivery Systems;206
11.1;I. Introduction;206
11.2;II. Polymers as Physical Carriers of Drugs;209
11.3;III. Polymers as Chemical Carriers of Drugs;236
11.4;IV. Conclusions;259
11.5;References;260
12;Chapter 6. The Design of Biocompatible Polymers;264
12.1;I. Introduction;264
12.2;II. Biocompatibility;267
12.3;III. Passive Tissue Implants;269
12.4;IV. Blood Compatible Polymers;277
12.5;References;284
13;Chapter 7. The Design of Insect Repellents;290
13.1;I. Introduction and Background;290
13.2;II. Design Concepts;296
13.3;III. Future Trends in Repellent Development;313
13.4;References;315
14;Chapter 8. Multivariate Data Analysis in Structure–Activity Relationships;320
14.1;I. Multivariate Data Analysis and Statistics;321
14.2;II. Multivariate Models of Dependence;322
14.3;III. Multivariate Models of Interdependence;326
14.4;IV. Program DATASCOPE for Multivariate Data Analysis;332
14.5;V. Applications of Multivariate Data Analysis;339
14.6;VI. Conclusion;352
14.7;ACKNOWLEDGEMENTS;353
14.8;References;353
15;Chapter 9. The Masca Model of Pharmacochemistry: II. Rational Empiricisms in the Multivariate Analysis of Opioids;356
15.1;I. Introduction;357
15.2;II. Blood-Brain Barrier;358
15.3;III. Morphinomimetic Polypeptides, Opioid Receptor Activity, and Correlation with Analgesia;363
15.4;IV. Discrimination of Structure–Analgesic and Structure-Antidiarrheal Relationships;365
15.5;V. Albumin Binding;367
15.6;VI. Recognition of Analgesics That Are of Special Interest in Multivariate Data Analysis;368
15.7;VII. Concluding Remarks;407
15.8;References;410
16;Index;416
17;Contents of Other Volumes;440