Drug Design

Drug Design

Medicinal Chemistry: A Series of Monographs, Vol. 8

1st Edition - January 28, 1978

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  • Editor: E. J. Ariëns
  • eBook ISBN: 9781483216102

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Drug Design, Volume VIII covers a critical review and new extensions of quantitative methods in drug design, the design of particular types of agents, such as synthetic sweeteners, and selective ion binding compounds. The book discusses the advances in the methodology of quantitative drug design; the application of pattern recognition to drug design; and the design of controlled drug delivery systems. The text also describes the use of receptor binding as a tool in the development of new bioactive steroids; the design of synthetic sweeteners; and the prospective assessment of environmental effects of chemicals. The design of selective ion binding macrocyclic compounds and their biological applications are also encompassed. Chemists, pharmacologists, biochemists, and people involved in drug design and manufacture will find the book invaluable.

Table of Contents

  • List of Contributors


    Contents of Other Volumes

    Chapter 1. Advances in the Methodology of Quantitative Drug Design

    I. How Should the Original Lead Be Used in the Design of Analogs?

    II. Which Physical Properties Should Be Related to Potency?

    III. Calculation, Measurement, and Meaning of Partition Coefficients

    IV. Theoretical Compartment Models for the Relationship between Physical Properties and Biological Potency

    V. Mathematical Methods for the Analysis of QSAR

    VI. Overview


    Chapter 2. The Application of Pattern Recognition to Drug Design

    I. Introduction

    II. Pattern Recognition: Philosophy and Methodology

    III. Pattern Recognition Applications

    IV. Conclusions


    Chapter 3. The Design of Controlled Drug Delivery Systems

    I. Introduction

    II. Therapeutic Systems for Controlled Drug Delivery

    III. Two Therapeutic Systems for Clinical Use

    IV. The ALZET® Osmotic Minipump for Animal Studies

    V. Conclusions


    Chapter 4. Receptor Binding as a Tool in the Development of New Bioactive Steroids

    I. Introduction

    II. Characterization of Steroid Hormone Receptors

    III. Screening Methodology

    IV. Screening Results

    V. Conformation Studies

    VI. Correlation between Binding Affinity and Biological Potency

    VII. Conclusion


    Chapter 5. The Design of Synthetic Sweeteners

    I. Introduction

    II. Design Concepts

    III. Current and Future Trends


    Chapter 6. The Prospective Assessment of Environmental Effects of Chemicals

    I. Introduction

    II. Identification of the Problem

    III. Types of Tests To Be Carried Out

    IV. Choice of Test Organisms

    V. Setup of the Test Program

    VI. Areas for Further Research

    VII. Conclusions


    Chapter 7. Design of Selective Ion Binding Macrocyclic Compounds and Their Biological Applications

    I. Introduction

    II. Historical Perspective

    III. Nomenclature and Physical Properties

    IV. Biological Applications

    V. Synthesis

    VI. Organic Reactions

    VII. Structural Relationships

    VIII. Cation Selectivities

    IX. Potential of Macrocyclic Compounds as Drugs



Product details

  • No. of pages: 440
  • Language: English
  • Copyright: © Academic Press 1978
  • Published: January 28, 1978
  • Imprint: Academic Press
  • eBook ISBN: 9781483216102

About the Editor

E. J. Ariëns

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