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Drug Discovery and Development, Volume 1 Drug Discovery

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ISBN-10: 0471398489

ISBN-13: 9780471398486

Edition: 2006

Authors: Mukund S. Chorghade

List price: $179.95
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This two volume set provides a comprehensive account of the entire sequence of operations involved in discovering a drug through the actual delivery of the drug to clinicians and medical practitioners. Includes case studies of the discovery of erythromycin analogs (antibiotics), Tagamet, and Ultiva (remifentanil) Discusses the discovery of agents for the treatment and management of bacterial infections, Parkinson?s disease, psoriasis, ulcers and stomach pain, atopic dermatitis, asthma, and cancer Contains chapters on combinatorial chemistry, molecular biology-based drug discovery, genomics, and chemogenomics The first volume of this set thoroughly describes conceptualizing a drug,…    
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Book details

List price: $179.95
Copyright year: 2006
Publisher: John Wiley & Sons, Incorporated
Publication date: 6/16/2006
Binding: Hardcover
Pages: 476
Size: 7.40" wide x 10.30" long x 1.14" tall
Weight: 2.2
Language: English

From Patent to Prescription: Paving the Perilous Path to Profit
A Simple Solution to a Complex Problem
An Intriguing Patent Problem
Another Structural Insight
Medicinal Chemistry in the New Millennium: A Glance into the Future
Practice of Medicinal Chemistry
Emergence as a Formalized Discipline
Early Developments
Present Status
Examples Involving Site-Directed Mutagenesis
Latest Trends
Evolving Drug Discovery and Development Process
Working Defi nition for Medicinal Chemistry
Immediate- and Long-Term Roles for Medicinal Chemistry
Pursuing Efficacy
Gathering Positive, Neutral, and Negative SARs During HTS
Example Involving Multidrug Resistance of Anticancer Agents
Compound Libraries: Example of Working with Nature to Enhance Molecular Diversity
Assessing and Handling Molecular Conformation
Obtaining Chemically Correct 3D Structures
Infl uence of Biological Environments: Example Involving Drug Metabolism
Dynamic Energy Relationships: Example Involving a Small Ring System
Druglike Properties and Privileged Structures
Tiered Structural Information and Searching Paradigms
ADMET Considerations
Assuring Absorption
Directing Distribution
Herbal Remedies: Example of Working with Nature to Discover
ADMET-Related Synergies, 59
Brute Force HTS to Uncover Multicomponent Synergies
Controlling Metabolism: Example Involving a Soft Drug Strategy
Optimizing Excretion
Avoiding Toxicity
Weighting Decision Criteria from Effi cacy and ADMET SAR
Process Chemistry Considerations
Cost and Green Chemistry
Defi ning Stereochemistry: Example Involving Benzylamine Chiral Auxiliary Synthetic Reagents
Analytical Chemistry/X-ray Diffraction
Latest Trends
Examples Involving Dopamine Receptors, c-AMP Phosphodiesterase Enzymes, and the Dynamics of Protein Folding
General Points
Attributes of Drug Discovery Libraries, Compound Hits, and Lead Compounds
Formalized Instruction of Medicinal Chemistry
Intellectual Property Considerations
Knowledge Versus Diversity Paradox
References and Notes
Contemporary Drug Discovery
Getting Started
Characteristics of a Suitable Lead Substance
Potency and Selectivity
Structure-Activity Relationships
Changing Appellation of the Best in Series: Analog Attrition
Some Criteria That a Hit Must Satisfy to Become a Drug
Level of Potency
Comparison of Potency and Efficacy
Druglike Character
Effi cacy Following Oral Administration
Lipinski Rules for Oral Absorption
Injectable Medications
Serum Protein Binding
Pharmaceutical Properties
Idiosyncratic Problems
Example of Drug Development That Illustrates Many of the Aforementioned Considerations