Drug Design (eBook)

Medicinal Chemistry: A Series of Monographs, Vol. 5

E. J. Ariens (Herausgeber)

eBook Download: PDF

2013 | 1. Auflage
374 Seiten
Elsevier Science (Verlag)
978-1-4832-1607-2 (ISBN)

Infos

Drug Design, Volume V covers the fundamental approaches to the development of bioactive compounds. The book discusses the utilization of operational schemes for analog synthesis in drug design; the design of enzyme inhibitors (transition state analogs); and the significance of structure-absorption-distribution relationships for drug design. The text describes the role of charge-transfer processes in the action of bioactive materials, as well as the approaches to the rational combination of antimetabolites for cancer chemotherapy. The physicochemical, quantum chemical, and other theoretical techniques for the understanding of the mechanism of action of central nervous system (CNS) agents, such as psychoactive drugs, narcotics, and narcotic antagonists and anesthetics, are also encompassed. Chemists, biochemists, pharmacologists, and people involved in drug design will find the book invaluable.

Inhalt

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. Utilization of Operational Schemes for Analog Synthesis in Drug Design 20
I. Introduction 20
II. Operational Scheme for Aromatic Substitution 21
III. Operational Scheme for Side Chains 27
IV. Examples 30
V. Rational Follow-up to the Schemes 38
VI. Conclusion 39
References 40
Chapter 2. The Design of Enzyme Inhibitors: Transition State Analogs 42
I. Introduction 43
II. Theory of the Transition State Analog Approach 44
III. Transition State Analogs 51
IV. Natural Transition State Analog Inhibitors 87
V. Synthetic Enzymes 93
References 95
Chapter 3. Structure-Absorption-Distribution Relationships: Significance for Drug Design 100
I. Introduction 100
II. The Earlier Hypotheses Relating to the Membrane Permeability or Pharmacological Activity with Partition Coefficients 101
III. Quantitative Correlations Using Multiple Regression Analysis and Substituent Constants 103
IV. Summary 146
References 147
Chapter 4. The Role of Charge-Transfer Processes in the Action of Bioactive Materials 152
I. Introduction 152
II. Fundamentals of the Charge-Transfer Process 154
III. Charge Transfer in Biological Systems 159
IV. Summary 181
References 183
Chapter 5. Approaches to the Rational Combination of Antimetabolites for Cancer Chemotherapy 188
I. General Introduction 189
II. Intracellular Metabolic Interactions 191
III. Alterations in Intracellular Metabolism 237
IV. Transport or Uptake Interactions 245
V. Scheduling 250
VI. Remote Systemic Biotransformation 251
VII. Modification of Host Nutrients and Toxicity 255
VIII. Non metabolic Combinations 261
IX. Concluding Remarks 263
References 264
Chapter 6. Physicochemical, Quantum Chemical, and Other Theoretical Techniques for the Understanding of the Mechanism of Action of CNS Agents: Psychoactive Drugs,Narcotics, and Narcotic Antagonists and Anesthetics 270
I. Introduction 271
II. Evaluation of Quantum Chemical Computational Methods 275
III. Psychoactive Drugs 295
IV. Narcotics and Narcotic Antagonists 320
V. Anesthetics 343
VI. Recent Developments in Sensitive Methods of Analyses for Normal Neurotransmitters and Their Metobolites 348
VII. Overall Perspective 350
References 352
Index 360

Produkt-Details

• Erscheint lt. Verlag: 22.10.2013
• Sprache: englisch
• Themenwelt: Medizin / Pharmazie ► Gesundheitsfachberufe
• Themenwelt: Medizin / Pharmazie ► Medizinische Fachgebiete ► Pharmakologie / Pharmakotherapie
• Themenwelt: Studium ► 2. Studienabschnitt (Klinik) ► Pharmakologie / Toxikologie
• ISBN-10: 1-4832-1607-1 / 1483216071
• ISBN-13: 978-1-4832-1607-2 / 9781483216072