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Textbook of Drug Design and Discovery, Third Edition

Edited by Tommy Liljefors, Povl Krogsgaard-Larsen, Ulf Madsen

Published July 25th 2002 by CRC Press – 592 pages

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Description

Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine.

The book follows drug design from the initial lead identification through optimization and structure-activity relationship with reference to the final processes of clinical evaluation and registration. Chapters investigate the design of enzyme inhibitors and drugs for particular cellular targets such as ion channels and receptors, and also explore specific classes of drug such as peptidomimetics, antivirals and anticancer agents. The use of gene technology in pharmaceutical research, computer modeling techniques, and combinatorial approaches are also included.

Reviews

"Describing all facets of modern drug design and development, this major textbook is an invaluable source of information for students of chemistry, phamacology, pharmacy, medicinal chemistry, medicine and biochemistry at all levels…Almost every page is illustrated with figures, tables and structural formulae."

Unlisted Drugs

"A well-structured and informative book…"

S. Damment, Glaxo, Newsletter of British Society for Toxicology

"Excellent book…The editors set a high standard."

Professor Graham Johnston, TiPS

"…a good and substantial book…good introductions to many aspects of a complex subject…"

Chris Ramsden, Chemistry and Industry

Contents

DRUG DESIGN AND DISCOVERY: AN OVERVIEW

Lester A. Mitscher

Introduction

Historical Perspective

What Kinds of Compounds Become Drugs?

Preparation and Organization for Drug Seeking

Sources of Hits, Leads, and Candidate Drugs

Lead Optimization

Cell Biology and Genomics as a source of Drug Targets

Future Developments

ROLE OF MOLECULAR RECOGNITION IN DRUG DESIGN

Peter Andrews and Michael Dooley

Introduction

Thermodynamic Considerations of Drug Binding

The Physical Basis of Intermolecular interaction

The Total Energy of Intermolecular interaction

Estimating Individual Group Components in Ligand-Receptor Interactions and Co-

Operativity

Some Rules of Thumb

STEREOCHEMISTRY IN DRUG DESIGN

Ian J. Kennedy and David E. Jane

Introduction

What Are Stereoisomers?

The Origin of Stereospecificity in Molecular Recognition

Why is Stereochemistry Important in Drug Design?

Methods of Obtaining Pure Stereoisomers

Analytical Methods of Determining Purity of Stereoisomers

COMPUTER-AIDED DEVELOPMENT OF THREE-DIMENSIONAL PHARMACOPHORE MODELS

Tommy Liljefors and Ingrid Petterson

Structure-and Pharmacophore-Based Ligand Design

The Pharmacophore Concept

Basic Principles and a Step-By-Step Procedure

Pharmacophore Elements and Their Representations

The Receptor-Bound or 'Active' Conformation

Molecular Superimposition

Receptor-Excluded and Receptor-Essential Volumes

Solvation Effects

Examples of 3D-Pharmacophore Models and Their Use

QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS AND EXPERIMENTAL DESIGN

Ulf Norinder and Thomas Hoberg

Introduction

Hansch Analysis

Physico-Chemical Properties

Applications of Hansch Equations

Pattern Recognition

3D-QSAR Methodologies

Experimental Design

RECEPTORS: STRUCTURE, FUNCTION AND PHARMACOLOGY

Hans Brauner-Osborne

Introduction

Receptor Structure and Function

Receptor Pharmacology

Related Subjects

  1. Pharmacology

Name: Textbook of Drug Design and Discovery, Third Edition (Paperback)CRC Press 
Description: Edited by Tommy Liljefors, Povl Krogsgaard-Larsen, Ulf Madsen. Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy,...
Categories: Pharmacology