Drug Design
Medicinal Chemistry: A Series of Monographs, Vol. 2
- 1st Edition - January 28, 1972
- Imprint: Academic Press
- Editor: E. J. Ariëns
- Language: English
- Paperback ISBN:9 7 8 - 1 - 4 8 3 2 - 0 2 6 1 - 7
- eBook ISBN:9 7 8 - 1 - 4 8 3 2 - 1 6 0 4 - 1
Drug Design, Volume II covers the design of bioactive compounds interacting with enzymes and playing a role in enzyme synthesis. The book discusses the modulation of… Read more
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Request a sales quoteDrug Design, Volume II covers the design of bioactive compounds interacting with enzymes and playing a role in enzyme synthesis. The book discusses the modulation of pharmacokinetics by molecular manipulation; the factors in the design of reversible and irreversible enzyme inhibitors; and the design of organophosphate and carbamate inhibitors of cholinesterases. The text also describes the design of reactivators for irreversibly blocked acetylcholinesterase; drug design based on the inhibition of protein synthesis in the context of susceptible enzymic reactions; as well as the role of enzymes and their synthesis as a target for antibiotic action. The rational design of antiviral agents; the design of penicillin; the design of peptide hormone analogs; as well as the advances in the design of diuretics are also considered. The book further tackles the design of biologically active steroids; the rational elements in the development of superior neuromuscular blocking agents; and the design of tumor-inhibitory alkylating drugs. Pharmacologists, chemists, and people involved in drug design will find the book invaluable.
List of Contributors
Preface
Introduction
Contents of Other Volumes
Chapter 1. Modulation of Pharmacokinetics by Molecular Manipulation
I. Introduction
II. The Significance of the Chemical Structure of Bioactive Compounds with Regard to the Various Processes Involved in Pharmacokinetics
III. Dissection of the Drug Molecule in Biofunctional Moieties
IV. Modulation of the Distribution of Pharmaca over the Various Compartments in Individual and Environmental Pharmacokinetics by Molecular Manipulation
V. Modulation of the Time-Concentration Relationship in the Distribution of Drugs by Molecular Manipulation
VI. Summary
References
Chapter 2. Factors in the Design of Reversible and Irreversible Enzyme Inhibitors
I. Introduction
II. Mechanism of Action of Selected Drugs
III. Factors Involved in the Reversible Inhibition of Selected Enzymes
IV. Irreversible Inhibition of Selected Enzymes
V. Kinetics of Irreversible Enzyme Inactivation
VI. Tissue-Specific Irreversible Enzyme Inhibitors
VII. Summary
References
Chapter 3. The Design of Organophosphate and Carbamate Inhibitors of Cholinesterases
I. Introduction
II. The Structure of the Active Zone of Cholinesterases
III. Design of Organophosphates
IV. Design of Carbamates
V. Future Approaches to Design of Anticholinesterases
References
Chapter 4 . The Design of Reactivators for Irreversibly Blocked Acetylcholinesterase
Text
References
Chapter 5. Inhibition of Protein Biosynthesis: Its Significance in Drug Design
I. Introduction
II. Protein Biosynthesis
III. Inhibitors of Protein Synthesis
TV. Design of Antibacterial Agents
V. Design of Amebicidal Agents
VI. Design of Antitumor Agents
VII. Design of Emetic Agents
VIII. Design of Antiviral Agents
IX. Conclusions
References
Chapter 6. Enzymes and Their Synthesis as a Target for Antibiotic Action
I. Introduction
II. Competitive Inhibitors of Enzymes
III. Irreversible Inhibitors or Enzymes as Antibacterial Agents
IV. Conclusion
References
Chapter 7. The Rational Design of Antiviral Agents
I. Introduction
II. Approaches to the Design of Antiviral Agents
III. Conclusions
References
Chapter 8. Design of Penicillins
I. Introduction
II. Effect of Penicillins on Bacteria
III. Behavior of Penicillins In Vivo
IV. Derivatives Which Liberate Penicillins In Vivo
V. Concluding Remarks
References
Chapter 9. The Design of Peptide Hormone Analogs
I. Introduction
II. Structural Aspects of Design
III. Biological Aspects and Practical Aims of Design
IV. Conclusions
References
Chapter 10. Recent Advances in the Design of Diuretics
I. Introduction
II. Mono- and Bicyclic Nitrogen Heterocycles
III. Sulfonamides and Disulfonamides
IV. α,β-Unsaturated Ketone Derivatives
V. Miscellaneous Group
References
Chapter 11. Design of Biologically Active Steroids
I. Introduction
II. Chemical Exploration and Pharmacological Screening
III. The Biological Study of the Cause of Disease
References
Chapter 12. Rational Elements in the Development of Superior Neuromuscular Blocking Agents
I. Introduction
II. Grosser Morphological Features Influencing the Response to Neuromuscular Blocking Agents
III. The Anatomy and Physiology of the Neuromuscular Junction
IV. Mechanisms of Neuromuscular Blockade
V. Clinically Desirable Features in a Neuromuscular Blocking Agent
VI. Relationships between Chemical Constitution and Neuromuscular Blocking Activity
VII. Rational Applications of Structure-Action Relationships to the Synthesis of New Neuromuscular Blocking Agents
VIII. Conclusion
References
Chapter 13. The Design of Tumor-Inhibitory Alkylating Drugs
I. Introduction
II. Types of Alkylating Groups
III. Sites of Reaction and Correlation with Biological Effects
IV. General Structural Considerations
V. Number of Reactive Centers
VI. Naturally Occurring Compounds and Analogs as Carriers of Alkylating Groups
VII. Dual Antagonists
VIII. Alkylating Agents Capable of Being Activated or Potentiated
IX. The Application of pH Differences
X. Compounds Designed for Intraarterial Infusion
XI. Conclusion
References
Author Index
Subject Index
- Edition: 1
- Published: January 28, 1972
- No. of pages (eBook): 666
- Imprint: Academic Press
- Language: English
- Paperback ISBN: 9781483202617
- eBook ISBN: 9781483216041
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