Pharmaceutical Book from C.H.I.P.S.

Drug Discovery and Development
Volume 1

Drug Discovery
edited by Mukund S. Chorghade

Drug Discovery and Development Volume 1 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


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
  • 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
  • Chemoinformatics
  • 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
  • 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
  • Attributes of Drug Discovery Libraries, Compound Hits, and Lead Compounds
  • Formalized Instruction of Medicinal Chemistry
  • Intellectual Property Considerations
  • Knowledge Versus Diversity Paradox

Contemporary Drug Discovery

  • Characteristics of a Suitable Lead Substance
  • Potency and Selectivity
  • Structure–Activity Relationships
  • Toxicity
  • 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
  • Distribution
  • Serum Protein Binding
  • Metabolism
  • Distribution
  • Excretion
  • Patenting
  • Pharmaceutical Properties
  • Idiosyncratic Problems
  • Example of Drug Development That Illustrates Many of the Aforementioned Considerations
  • Control of Blood Pressure with Drugs
  • Historical Background
  • Finding a Starting Point: A Clue from Nature
  • Renin–Angiotensin–Aldosterone System
  • Attempts to Inhibit Renin
  • Attempts to Inhibit Angiotensin-Converting Enzyme
  • Peptides Make Poor Orally Active Drugs
  • Analoging Studies of Pit Viper–Inspired Peptides
  • Peptidomimetics
  • Adaptation to Inhibition of ACE
  • Success Inspires Competition
  • Taking a Different Approach
  • Analoging to Enhance Absorption
  • Clinical SAR

Combinatorial Chemistry in the Drug Discovery Process

  • The Birth of Combinatorial Chemistry
  • Development of Screening Strategies for Libraries
  • From Peptides to Small Molecule Synthesis
  • Beyond Solid-Phase Chemistry
  • The Role of Combinatorial Chemistry in Drug Discovery
  • Designing Combinatorial Libraries
  • Describing and Measuring Diversity
  • A More Focused Approach
  • Tools for Synthesis of Combinatorial Libraries
  • Nonautomated Tools
  • Mix-and-Sort Systems
  • Automated Synthesizers
  • Postsynthesis Processing
  • Managing the Combinatorial Process
  • Specifi cation of Combinatorial Libraries
  • Controlling the Automated Workflow
  • From Specialist Discipline to Standard Tool
  • Application of Combinatorial Chemistry in Drug Discovery

Parallel Solution-Phase Synthesis

  • Recent Reports of Parallel Solution-Phase Synthesis
  • Solid Supported Reagents, Scavengers, and Catalysts

Timing of Analog Research in Medicinal Chemistry

  • Early Phase Analogs
  • ACE Inhibitors
  • AT1 Antagonists
  • Proton Pump Inhibitors
  • Insulin Sensitizers: Glitazones
  • HMG-CoA Reductase Inhibitors
  • Antimigraine Drugs
  • Drug Analogs
  • Metoclopramide Analogs
  • Azatadine Analogs
  • Miconazole Analogs
  • Nifedipine Analogs
  • Propranolol Analogs
  • Clodronate Analogs

Possible Alternatives to High-Throughput Screening

  • Analog Design
  • Pharmacophere-Based Analog Design: Scaffold Hopping or Scaffold Morphing
  • Natural Compounds as Models
  • Emergence of New Activities
  • Physiopathological Hypotheses
  • Discovery of Levodopa
  • H2-Receptor Antagonists
  • Rimonabant and Obesity
  • Contributions from Clinical Investigations
  • New Leads from Old Drugs: The SOSA Approach

Proteomics and Drug Discovery

  • Drug Discovery Process
  • Motivation for Improvement
  • High-Throughput Screening Approaches to Drug Discovery
  • Emerging Technologies and Approaches: Scale and Speed
  • Genomics
  • Proteomics
  • Functional Areas of Proteomics
  • Fractionation and Purification
  • Identification
  • Quantitation
  • Characterization
  • Protein Chip Technology
  • Issues Addressed
  • Current State of the Technology
  • Proteomics Data Analysis: Computational Biology and Bioinformatics
  • Proteomics and Drug Discovery
  • Target Identification
  • Target Validation
  • Screening for Hits
  • Lead Optimization
  • Pharmacology and ADME-Tox
  • Clinical Trials: Biomarkers and Pharmacogenomics

Using Drug Metabolism Databases During Drug Design and Development

Discovery of the Antiulcer Drug Tagamet

  • Pharmacological Receptors
  • Peptic Ulcer Disease
  • Search for New Antiulcer Drugs
  • Search for an H2-Receptor Histamine Antagonist
  • Histamine Receptors
  • Biological Approach to a Histamine Antagonist at Non-H1 Receptors
  • Chemical Approach to an Antagonist: Generating a Lead
  • Lead Optimization
  • Validating the Research Program
  • Development of a Clinical Candidate Drug
  • Dynamic Structure–Activity Analysis
  • Imidazole Tautomerism and Sulfur Methylene Isosterism
  • Isosteres of Thiourea and the Discovery of Cimetidine
  • Cimetidine: A Breakthrough in the Treatment of Peptic Ulcer Disease

Discovery of Potent Nonpeptide Vasopressin Receptor Antagonists

  • Genesis of the Vasopressin Receptor Antagonist Project
  • Vasopressin, Its Receptors, and Disease
  • The Game Plan
  • Novel Chemotypes: Variations on a Theme
  • Azepinoindoles
  • Bridged Bicyclic Derivatives
  • Thiazino-, Oxazino-, and Pyrazinobenzodiazepines

Discovery and Development of the Ultrashort-Acting Analgesic Remifentanil

  • Discovery of Remifentanil
  • Chemical Development of Remifentanil
  • Human Clinical Trials with Remifentanil

Discovery and Development of Nevirapine

  • Lead Discovery and Optimization
  • Chemical Development and Process Research
  • Mechanism of Action

Applications of Nuclear Imaging in Drug Discovery and Development

  • Process and Challenges of Drug Development
  • Role and Contribution of Position Emission Tomography
  • Principles and Evolution of Technology
  • Introduction to PET Principles
  • Suitable Targets
  • Suitable Animal Models
  • Role in Drug Discovery
  • Target Validation and Drug Design
  • Preclinical Studies

Polymeric Sequestrants as Nonabsorbed Human Therapeutics

  • Polymers as Specifi c Molecular Sequestrants
  • Sequestration of Inorganic Ions in the GI Tract
  • Polymeric Potassium Sequestrants: A Nonabsorbed Therapy for Hyperkalemia
  • Polymeric Drugs for Chronic Renal Failure
  • Polymeric Iron Sequestrants for the Treatment of Iron Overload Disorders
  • Sequestration of Bile Acids: Polymers as Cholesterol-Lowering Agents
  • Sequestration of Pathogens: Polymeric Anti-infective Agents
  • Sequestration of Toxins
  • Polymeric Antimicrobial Agents

Botanical Immunomodulators and Chemoprotectants in Cancer Therapy

  • Immunomodulation
  • Ethnopharmacology and Botanical Immunomodulators
  • Adaptogens or Adjustive Medicine
  • Botanicals with Adaptogenic Activity
  • Rasayana Botanicals as Adaptogens
  • Chemoprotection
  • Drug Targets and Current Trends
  • Chemoprotectants for Antimetabolites
  • Thiol-Based Chemoprotectants for Cisplatin and Oxazophosphorine-Based Alkylating Agents
  • Chemoprotectants for Anthracyclines
  • Botanical Immunomodulators as Chemoprotectants
  • Radioprotection
  • Radioprotectants from Botanicals
  • Botanical Immunomodulators as Antitumor Agents


Also available:
Drug Discovery and Development Volume 2: Drug Development
Drug Discovery and Development 2-Volume Set

click here to see books of related interest


Drug Discovery and Development Volume 1
Drug Discovery
edited by Mukund S. Chorghade

2006 • 476 pages • $132.00 + shipping
Texas residents please add 6.75 % sales tax

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