Drug Design - 1st Edition - ISBN: 9780120603022, 9781483216041

Drug Design

1st Edition

Medicinal Chemistry: A Series of Monographs, Vol. 2

Editors: E. J. Ariëns
eBook ISBN: 9781483216041
Imprint: Academic Press
Published Date: 28th January 1972
Page Count: 666
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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 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.

Table of Contents

List of Contributors



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


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


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


Chapter 4 . The Design of Reactivators for Irreversibly Blocked Acetylcholinesterase



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


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


Chapter 7. The Rational Design of Antiviral Agents

I. Introduction

II. Approaches to the Design of Antiviral Agents

III. Conclusions


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


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


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


Chapter 11. Design of Biologically Active Steroids

I. Introduction

II. Chemical Exploration and Pharmacological Screening

III. The Biological Study of the Cause of Disease


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


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


Author Index

Subject Index


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© Academic Press 1971
Academic Press
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About the Editor

E. J. Ariëns

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