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    Medicinal chemistry : the modern drug discovery process / Erland Stevens.

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    • Title:Medicinal chemistry : the modern drug discovery process / Erland Stevens.
    •    
    • Variant Title:Modern drug discovery process
    • Author/Creator:Stevens, Erland.
    • Published/Created:Boston : Pearson, ©2014.

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    • Library of Congress Subjects:Pharmaceutical chemistry.
      Drug delivery systems.
    • Medical Subjects: Chemistry, Pharmaceutical.
      Drug Delivery Systems.
      Drug Discovery.
      Pharmaceutical Preparations--chemistry.
    • Description:xiii, 418 pages : illustrations ; 26 cm.
    • Series:Pearson advanced chemistry series.
    • Notes:Includes bibliographical references and index.
    • ISBN:9780321710482 (Student edition)
      0321710487 (Student edition)
    • Contents:Machine generated contents note: ch. 1 Brief History of Drug Discovery
      1.1. Selected Drugs from Early Recorded History
      China
      India
      Middle East
      Greek, Roman, and Byzantine Periods
      1.2. Middle Ages to Modern Times
      Natural Products
      Advances in Inorganic Chemistry
      Sulfa Drugs
      1.3. Evolution of the U.S. Food and Drug Administration
      Corporate Self-Regulation
      Food, Drug, and Cosmetic Act of 1938
      Continuing Challenges and Refinements
      Summary
      References
      ch. 2 Modern Drug Discovery Process
      2.1. Market Analysis
      Case Study Treatment of Acid Reflux
      2.2. Target Selection
      Finding a Target
      Traditional Methods
      Case Study ACE Inhibitors and A-II Receptor Blockers
      Case Study HMG-CoA Reductase Inhibitors
      Assay Development
      2.3. Lead Discovery
      2.4. Lead Optimization
      2.5. Patent Filing
      2.6. Animal Trials
      2.7. Investigational New Drug Application
      2.8. Phase Trials
      Phase I
      Phase II
      Phase III
      2.9. New Drug Application
      2.10. Launch
      2.11. Additional Considerations
      Accelerated Approval
      Generic Drugs
      Approval Outside the United States
      Summary
      Questions
      References
      ch. 3 Trip through the Body
      3.1. Complexity of the Body
      What Is the Body?
      Organization of the Body
      Balance of Life
      3.2. Absorption: Drug Entry into the Bloodstream
      Oral
      Injection
      Transdermal
      Other Routes
      Topical
      3.3. Distribution: Drug Transport
      Blood
      Crossing Membranes
      Blood-Brain Barrier
      3.4. Pharmacodynamics: At the Drug Target
      3.5. Metabolism and Elimination: Drug Removal
      Kidneys
      Liver
      Other Routes
      Summary
      Questions
      References
      ch. 4 Enzymes as Drug Targets
      4.1. Introduction to Enzymes
      Definition
      Structure
      Case Study Use of a-Helices to Cross Cell Membranes
      Types
      4.2. Mode of Action
      Theory
      Regulation
      4.3. Kinetics
      Single Substrate
      Multiple Substrates
      4.4. Inhibitors
      Reversible
      Irreversible
      4.5. Pharmaceutical Concerns
      Ki and IC50
      Mutational Resistance to Inhibitors
      Concentration Effects
      Metabolism of Drugs
      Summary
      Questions
      References
      ch. 5 Receptors as Drug Targets
      5.1. Receptors
      Similarities to Enzymes
      Differences from Enzymes
      5.2. Receptor Classification
      Ligand-Gated Ion Channels
      G-Protein-Coupled Receptors
      Tyrosine Kinase-Linked Receptors
      Nuclear Receptors
      5.3. Types of Ligands
      Agonists
      Antagonists
      Inverse Agonists
      5.4. Receptor Theories
      Occupancy Theory
      Allosteric Theory
      Rate Theory
      Drug-Target Residence Time
      Summary
      Questions
      References
      ch. 6 Oligonucleotides as Drug Targets
      6.1. Basics of Nucleic Acids
      Building Blocks of Nucleic Acids
      DNA
      RNA
      6.2. Common Methods of Oligonucleotide Recognition
      Base Pairing
      Charge-Charge Interactions
      Intercalation
      Groove Binding
      6.3. Interference with Nucleic Acid Synthesis and Function
      Anti-HIV Nucleic Acid Analogues
      Nucleic Acid Antimetabolites
      Tubulin Interactions
      Summary
      Questions
      References
      ch. 7 Pharmacokinetics
      7.1. Intravenous Bolus
      Cp vs. Time and Elimination
      Clearance
      Volume of Distribution
      Serum Binding
      Case Study Minimization of Serum Binding
      7.2. Intravenous Infusion
      Infusion Rate Constant
      Loading Bolus
      Infusion-Like Administration Routes
      7.3. Oral
      Absorption and Elimination Phases
      Bioavailability
      Absorption Rate Constant
      Multiple Oral Doses
      Clearance and Volume of Distribution Revisited
      Case Study Fast Onset Sertraline Analogues
      7.4. Drug Metabolites
      Summary
      Questions
      References
      ch. 8 Metabolism
      8.1. Introduction
      8.2. Metabolic Reactions
      Phase I Reactions
      Phase II Reactions
      8.3. Metabolism Issues
      Metabolite Activity
      Case Study Sertraline and Later Generation SSRIs
      Case Study Acetaminophen
      Case Study MPPP
      Inhibition of Metabolism by Drugs
      Case Study Cimetidine
      Case Study St. John's Wort
      Population Variations
      Case Study Theophylline
      8.4. Prodrugs
      Case Study Clopidogrel and Prasugrel
      Summary
      Questions
      References
      ch. 9 Molecular Structure and Diversity
      9.1. Determining Target Structure
      Literature
      X-Ray Crystallography
      NMR Spectroscopy
      Molecular Modeling
      Case Study Protease Inhibition in Coronaviruses
      9.2. Complementarity between a Target and Drug
      Intermolecular Forces
      Molecular Shape
      Case Study Conformational and Stereochemical Effects on Ligands of Acetylcholine Receptors
      Drug Pharmacophore
      9.3. Searching for Drugs
      Diversity and Molecular Space
      Privileged Structures
      9.4. Combinatorial Chemistry
      Parallel Synthesis
      Split Synthesis
      Advantages and Disadvantages
      Summary
      Questions
      References
      ch. 10 Lead Discovery
      10.1. Approaches to Searching for Hits
      Traditional Library Screening
      Fragment-Based Screening
      Case Study Inhibition of Stromelysin
      Case Study Inhibition of Cyclin-Dependent Kinase 2
      Case Study Inhibition of Acetylcholine Esterase
      Virtual Screening
      Case Study Inhibition of Protein Kinase B
      Case Study Inhibition of Sir2 Type 2
      Case Study C-C Chemokine Receptor Type 5 Agonists
      10.2. Filtering Hits to Leads
      Pharmacodynamics and Pharmacokinetics
      Biological Assays
      Lipinski's Rules and Related Indices
      Final Concerns for Promotion of a Hit to a Lead
      10.3. Special Cases
      Serendipity
      Case Study Penicillin
      Case Study Chlordiazepoxide
      Clinical Observations
      Case Study Viloxazine
      Case Study Sildenafil
      Natural Products
      Summary
      Questions
      References
      ch. 11 Lead Optimization: Traditional Methods
      11.1. Pharmacophore Determination
      Case Study The Pharmacophore of Morphine
      Case Study The Pharmacophore of Migrastatin, a Promising Anticancer Compound
      11.2. Functional Group Replacements
      11.3. Alkyl Group Manipulation
      Chain Homologation
      Ring-Chain Interconversion
      11.4. Isosteres
      Case Study Cimetidine
      Case Study Extension of the Half-Life of Iloprost
      Case Study Deuteration of Vanlafaxine
      11.5. Directed Combinatorial Libraries
      Case Study Raf Kinase Inhibitors
      11.6. Peptidomimetics
      Case Study Angiotensin-Converting Enzyme Inhibitors
      Case Study Human Immunodeficiency Virus-1 Protease Inhibitors
      Summary
      Questions
      References
      ch. 12 Lead Optimization: Hansch Analysis
      12.1. Background
      12.2. Parameters
      Hammett Constants: An Electronic Parameter
      Hansch Constants: A Lipophilicity Parameter
      Taft Steric Parameter
      Other Parameters
      12.3. Hansch Equations
      Case Study Phosphonate Ester Cholinesterase Inhibitors
      Case Study Carboxylate Antifungals
      Case Study Tumor Cell Resistance Modulators
      12.4. Craig Plots
      12.5. Topliss Trees
      12.6. Evaluating Hansch Analysis
      12.7. Comparative Molecular Field Analysis
      Case Study Comparing Hansch Analysis and CoMFA
      Summary
      Questions
      References
      ch. 13 Aspects in Pharmaceutical Synthesis
      13.1. Solids, Solids, Solids
      Recrystallization
      Acid-Base Salts
      Case Study Salt Forms of RPR 200,735
      Cocrystals
      Case Study Itraconazole-Succinic Acid Cocrystal
      Polymorphs
      Case Study Polymorphs of Ritonavir
      13.2. Stereochemistry
      Resolution
      Case Study Resolution of Sertraline
      Asymmetric Synthesis
      13.3. Scale-Up: From Bench to Plant
      Case Study Fluvastatin
      Case Study Sildenafil
      13.4. Green Chemistry
      Principles of Green Chemistry
      Green Metrics
      Case Study Case Study and Sample Calculation: Ibuprofen
      Case Study Sildenafil
      13.5. Regulatory Issues
      Good Practices
      Impurities
      Generic Drugs and Patents
      Case Study Polymorphs of Ranitidine
      Summary
      Questions
      References
      Appendix A Top Selling Oral Drug Classes
      Appendix A.1 Allergic Rhinitis
      Appendix A.2 Bacterial Infection
      Appendix A.3 Cancer
      Appendix A.4 Clinical Depression
      Appendix A.5 Diabetes-Type 2
      Appendix A.6 Erectile Dysfunction
      Appendix A.7 Gastroesophageal Reflux Disorder
      Appendix A.8 Generalized Anxiety Disorder
      Appendix A.9 Hyperlipidemia
      Appendix A.10 Hypertension
      Appendix A.11 Pain
      Appendix A.12 Viral Infection
      Appendix B Performing Regressions with LINEST
      Appendix B.1 Equation 12.20
      Appendix B.2 Equation 12.21
      Appendix B.3 Equation 12.22.
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