Drug Design

Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 2

1st Edition - January 28, 1972

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  • Editor: E. J. Ariëns
  • eBook ISBN: 9781483216041

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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

Product details

  • No. of pages: 666
  • Language: English
  • Copyright: © Academic Press 1972
  • Published: January 28, 1972
  • Imprint: Academic Press
  • eBook ISBN: 9781483216041

About the Editor

E. J. Ariëns

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