Z700819 Sigma

Practice of Medicinal Chemistry, 2nd ed.

an essential handbook for the medicinal chemist - a complete guide to the drug discovery process

  •  ISBN-10 0-12-744481-5

  •  ISBN-13 978-0-12-744481-9


publication info   C. Wermuth, ed., Academic Press, 2003, 624 pp., hard cover


General description

This is an essential handbook for the medicinal chemist - a complete guide to the drug discovery process.

It reviews practical aspects of Medicinal Chemistry, emphasizing the daily problems when dealing with lead discovery/identification methodologies, with structure-activity relationship studies aimed to scale up potency and target selectivity, and when optimizing pharmacokinetic and pharmaceutical properties by means of ultimate chemical modifications.

This edition is revised, with around 30% new material, and refocussed to reflect the developments in genomics, proteomics, high throughput screening of compounds and drug solubilization.

Table of Contents

A Brief History Of Drugs; From Plant Extracts To DNA Technology:
Medicinal Chemistry: Definition And Objectives, The Three Main Phases Of Drug Activity, Drug And Diseases Classifications
Measurement And Expression Of Drug Effects
Drug Targets: Molecular Mechanisms Of Drug Action
Strategies In The Search For New Lead Compounds Or Original Working Hypotheses
Natural Products As Pharmaceuticals And Sources For Lead Structures
Basics Of Combinatorial Chemistry
The Contribution Of Molecular Biology To Drug Discovery
Electronic Screening: Lead Finding From Database Mining
High-Speed Chemistry Libraries: Assessment Of Drug-Likeness
Web Alert — Using The Internet For Medicinal Chemistry
Molecular Variations In Homologous Series: Vinylogues And Benzologues
Molecular Variations Based On Isosteric Replacements
Ring Transformations
Introduction Of Conformational Restriction And/Or Steric Hindrance
Identical And Non Identical Twin Drugs
Optical Isomerism In Drugs
Application Strategies For The Primary Structure-Activity Relationship Exploration
Specific Substituent Groups
The Role Of Functional Groups In Drug–Receptor Interactions
Compound Properties And Drug Quality
Quantitative Approaches To Structure-Activity Relationships
Structural Aspects Of Drug Action I
Pharmacophore Identification And Receptor Mapping
Three-Dimentional Quantitative Structure-Property Relationships
Protein Crystallography And Drug Discovery
Protein Comparative Modelling And Drug Discovery

The Transition From Agonist To Antagonist Activity:
Symmetry And Other Considerations
Design Of Peptidomimetics
The Fate Of Xenobiotics In Living Organisms
Biotransformation Reactions
Chemical Mechanisms Of Toxicity
Basic Knowledge For Designing Safer Drugs
Designing Prodrugs And Bioprecursors
Macromolecular Carriers For Drug Targeting
Preparation Of Water Soluble Compounds Through Salt Formation
Preparation Of Water-Soluble Compounds By Covalent Attachment Of Solubilizing Moieties
Drug Solubilization With Organic Solvents, Surfactants And Lipids
Improvement Of Drug Properties By Cyclodextrins
Chemical And Physicochemical Solutions To Formulation Problems
Discover A Drug Substance, Formulate And Develop It To A Product
Drug Nomenclature
Legal Aspects Of Product Protection
The Consumption And Production Of Pharmaceuticals

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