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Foye's Principles of Medicinal Chemistry
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Maintaining its status as the gold standard in medicinal chemistry education, Foye's Principles of Medicinal Chemistry, 9th Edition, presents a renewed focus on the fundamental concepts that form the backbone of this critical discipline. This latest edition, helmed by new senior editors Marc Harrold and Kim Beck, continues the text's legacy of excellence while streamlining content for today's pharmacy students and practitioners. Expert contributions from experienced educators, research scientists, and clinicians clarify the chemical basis of drug action, emphasizing the structure-activity relationships, physicochemical-pharmacokinetic properties, and metabolic profiles of the most commonly used drugs.UPDATED! Focused content emphasizes essential information in an ideal format for contemporary PharmD curricula.
UPDATED! Drug information equips students with the latest developments in drug discovery, structure optimization and clinical use.
Clinical Significance testimonials provide a clinician’s view of the relevance of medicinal chemistry to practice.
End-of-Chapter exercises provide valuable self-assessment opportunities and reinforce key concepts.
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Especialidad
- Bioquímica
Maintaining its status as the gold standard in medicinal chemistry education, Foye's Principles of Medicinal Chemistry, 9th Edition, presents a renewed focus on the fundamental concepts that form the backbone of this critical discipline. This latest edition, helmed by new senior editors Marc Harrold and Kim Beck, continues the text's legacy of excellence while streamlining content for today's pharmacy students and practitioners. Expert contributions from experienced educators, research scientists, and clinicians clarify the chemical basis of drug action, emphasizing the structure-activity relationships, physicochemical-pharmacokinetic properties, and metabolic profiles of the most commonly used drugs.UPDATED! Focused content emphasizes essential information in an ideal format for contemporary PharmD curricula.
UPDATED! Drug information equips students with the latest developments in drug discovery, structure optimization and clinical use.
Clinical Significance testimonials provide a clinician’s view of the relevance of medicinal chemistry to practice.
End-of-Chapter exercises provide valuable self-assessment opportunities and reinforce key concepts.
- Dedication
- Dedication to William O. Foye
- Preface
- Acknowledgements
- Contributors
- Clinical Contributors
- Contents
- Part I Principles
- Chapter 1 The Evolution of Medicinal Chemistry
- Discovery and Chemistry of Biologically Active Substances
- Evolution From Art to Science
- Biology-Enabled Chemistry and Vice Versa
- Selected Technology-Based Examples of Medicinal Chemistry Development
- Where Will Medicinal Chemistry Be in 2050?
- Summary
- Chapter 2 Foundational Principles and Functional Group Impact on Activity
- Introduction
- Relationship Between Molecular Structure and Biologic Activity
- Selectivity of Drug Action and Drug Receptors
- Physicochemical Properties of Drugs
- Relative Acid Strength (pKa)
- Drug Absorption
- Passive Diffusion
- Active Transport (Influx and Efflux Transporters)
- Prodrugs
- Stereochemistry and Drug Action
- Stereochemical Definitions
- Drug Design: Discovery and Structural Modification of Lead Molecules
- Peptide and Protein Drugs
- Summary
- Acknowledgments
- Chapter 3 Drug Metabolism
- Introduction
- Pathways of Metabolism
- Factors Affecting Metabolism
- Drug Biotransformation Pathway (Phase 1)
- Drug Conjugation Pathways (Phase 2)
- Elimination Pathways
- Drug Metabolism and Age
- Genetic Polymorphism
- First-Pass Metabolism
- Extrahepatic Metabolism
- Stereochemical Aspects of Drug Metabolism
- Metabolic Bioactivation: Role in Hepatotoxicity, Idiosyncratic Reactions, and Chemical Carcinogenesis
- Drug-Drug Interactions
- Gender Differences in Drug Metabolism
- Major Pathways of Metabolism
- Chapter 4 Membrane Drug Transporters
- Introduction
- Mechanisms of Membrane Transport
- Classification of Transporters
- Effect of Transport on Drug Pharmacokinetics and Drug-Drug Interactions
- Conclusions
- Chapter 5 Principles of Biotechnology-Derived Drugs
- Introduction
- Pharmacogenetics
- Pharmaceutical Biotechnology Methods
- General Properties of Biotechnology-Produced Medicinal Agents
- Monoclonal Antibodies
- Antibody-Drug Conjugates
- Pharmacogenomics and Personalized Medicine
- Gene Therapy
- Summary
- Part 2 Receptor Targets
- Chapter 6 G Protein–Coupled Receptors
- Introduction
- Transmembrane G Protein–Coupled Receptors
- Adrenoceptors
- Serotonin Receptors
- Cholinergic Muscarinic Receptors
- Opioid Receptors
- Histamine Receptors
- Dopamine Receptors
- Acknowledgments
- Chapter 7 Nuclear Receptors
- Introduction
- Nuclear Receptor Activation
- Estrogen Receptors
- Progesterone Receptors
- Androgen Receptors
- Glucocorticoid Receptors
- Mineralocorticoid Receptors
- Thyroid Receptors
- Peroxisome Proliferator–Activated Receptors
- Retinoic Acid Receptors
- Retinoid X Receptors
- Vitamin D Receptors
- Orphan Receptors
- Chapter 8 Ion Channel Receptors
- Introduction
- Ligand-Gated Ion Channels
- Voltage-Gated and Second Messenger–Gated Channels
- Mechanisms of Calcium Movement and Storage
- Acknowledgments
- Chapter 9 Enzyme/Catalytic Receptors
- Introduction
- Conclusion
- Part 3 Pharmacodynamic Agents
- Section 1 Drugs Impacting the Central Nervous System
- Chapter 10 Drugs Used to Treat Neuromuscular Disorders
- Overview of Neuromuscular Disorders
- Parkinson Disease
- Multiple Sclerosis
- Amyotrophic Lateral Sclerosis
- Duchenne Muscular Dystrophy
- Spinal Muscular Atrophy
- Spasticity Disorders
- Acknowledgment
- Chapter 11 Antipsychotic and Anxiolytic Drugs
- Overview of Antipsychotic and Anxiolytic Medicines
- Psychoses and Anxiety Disorders
- Schizophrenia
- Anxiety Disorders
- Chapter 12 Drugs Used to Treat Depression
- Introduction
- Types of Depressive Disorders
- Biologic Basis of Depression
- General Approaches to Treatment of Depression
- Antidepressants in Psychotherapy
- Effect of Physicochemical Properties and Stereochemistry on Antidepressant Efficacy
- Drug Metabolism and Drug-Drug Interactions
- Specific Drugs
- Electroconvulsive Therapy
- Chapter 13 Drugs Used to Treat Alzheimer Disease and Attention-Deficit/Hyperactivity Disorder
- Drugs Used to Treat Alzheimer Disease
- Drugs Used to Treat Attention-Deficit/Hyperactivity Disorder
- Acknowledgment
- Chapter 14 Drugs Used to Induce/Support Sedation or Anesthesia
- Agents That Induce or Promote Sedation and Sleep
- Agents that Induce or Maintain General Anesthesia
- Chapter 15 Drugs Used to Treat Seizure Disorders
- Overview of Seizure Disorders
- Physiologic Mechanisms Involved in Seizures
- Chemistry of Commonly Used Antiepileptic Drugs
- Antiseizure Medications in the Pipeline
- Section 2 Drugs Impacting Pain Perception
- Chapter 16 Drugs Used to Treat Pain: Centrally Acting Agents
- Pain
- Opioid Analgesics and Antagonists
- Peripherally Restricted µ Agonists: Antidiarrheals
- Drugs Used to Treat Neuropathic Pain
- Antimigraine Drugs
- Acknowledgment
- Chapter 17 Drugs Used to Treat Pain: Peripherally Acting Agents
- Introduction
- Inflammation
- General Gastrointestinal Considerations for Nonsteroidal Anti-inflammatory Drug Therapy
- Therapeutic Classifications
- Disease-Modifying Antirheumatic Drugs
- Drugs Used to Treat Gout
- Local Anesthetics
- Acknowledgments
- Section 3 Drugs Impacting the Cardiovascular System
- Chapter 18 Drugs Used to Treat Dyslipidemic Disorders
- Chemistry and Biochemistry of Plasma Lipids
- Therapeutic Overview
- Drugs Used to Treat Dyslipidemia
- HMG-CoA Reductase Inhibitors
- Cholesterol Absorption Inhibitor
- Proprotein Convertase Subtilisin/Kexin Type 9 Inhibitors
- Bempedoic Acid
- Bile Acid Sequestrants
- Orphan Drugs for the Treatment of Homozygous Familial Hypercholesterolemia
- Nicotinic Acid (Niacin)
- Fibrates
- ω-3 Fatty Acids
- Chapter 19 Drugs Used to Treat Hypertensive/Hypotensive Disorders
- Cardiovascular Hypertension
- Diuretics
- Renin-Angiotensin Pathway
- Calcium Channel Blockers
- Central and Peripheral Sympatholytics and Vasodilators
- Acknowledgments
- Chapter 20 Drugs Used to Treat Ischemic Heart Disease, Heart Failure, and Arrhythmias
- Drugs for the Treatment of Angina
- Drugs for the Treatment of Heart Failure
- Drugs for the Treatment of Cardiac Arrhythmia
- Chapter 21 Drugs Used to Treat Thrombotic Disorders
- Epidemiology and Economic Impact of Thrombotic Diseases
- Physiology of Hemostasis
- Pathophysiology of Thrombus Formation
- Antiplatelet Drugs
- Anticoagulants
- Antithrombotic/Profibrinolytic Oligonucleotide
- Fibrinolytic Drugs
- Thrombopoietin-Receptor Agonists
- Spleen Tyrosine-Kinase Inhibitor
- Fibrinolysis Inhibitors
- Section 4 Drugs Impacting Hormonal Systems
- Chapter 22 Drugs Used to Treat Diabetic Disorders
- Diabetes Mellitus: Historical Perspectives
- Chapter 23 Drugs Used to Treat Obesity
- Therapeutic Context
- Pharmacology Overview
- Chapter 24 Drugs Used to Treat Inflammatory and Corticosteroid Deficiency Disorders
- Introduction
- Steroid Nomenclature and Structure
- Mechanism of Steroid Hormone Action
- History and Disease States
- Biosynthesis
- Metabolism
- Physiologic Effects of Adrenocorticoids
- Summary of Structure-Activity Relationships
- Pharmacologic Effects and Clinical Applications
- Development of Adrenocorticoid Drugs
- Adrenocorticoid Antagonists
- Acknowledgment
- Chapter 25 Drugs Used to Advance Men’s and Women’s Health
- Introduction
- Sex Hormones
- Drugs Used in Modulating Women’s Fertility
- Drugs Used in Hormone Replacement Therapy for Menopause
- Drugs Used in the Treatment of Androgen Insufficiencies
- Drugs Used for the Treatment of Erectile Dysfunction
- Drugs Used for Benign Prostatic Hyperplasia
- Treating Skin Conditions With Inhibitors of the Androgen Receptor Axis
- Treatment of Prostatitis
- Drugs Used for the Treatment of Hormone-Dependent Cancers (Breast, Prostate)
- Testicular Cancer
- Acknowledgments
- Chapter 26 Drugs Used to Treat Thyroid Disorders
- Introduction
- Biosynthesis, Transport, Metabolism, and Excretion of Thyroid Hormones
- Physiologic Actions of Thyroid Hormones
- Thyroid Diseases and Therapeutic Interventions
- Acknowledgments
- Chapter 27 Drugs Used to Treat Calcium-Dependent Disorders
- Introduction
- Hormonal Regulation of Serum Calcium Levels
- Normal Physiology
- Disease States Associated With Abnormal Calcium Homeostasis
- Drug Therapies Used to Treat Osteoporosis
- PTH Analogues
- Drug Therapies Used to Treat Hyperparathyroidism
- Drug Therapies Used to Treat Hypercalcemia of Malignancy
- Drug Therapy Used in the Treatment of Hypoparathyroidism
- Section 5 Drugs Impacting Immune, Gastrointestinal and Genitourinary Systems
- Chapter 28 Drugs Used to Treat Gastrointestinal and Genitourinary Disorders
- Introduction
- Drugs Used for the Treatment of Gastrointestinal Disorders, Including Ulcer and Gastroesophageal Reflux Disease
- Antiemetic Agents
- Irritable Bowel Syndrome and Treatment Options
- Agents That Impact Gastrointestinal and Genitourinary Smooth Muscle and Glands
- Chapter 29 Drugs Used to Treat Allergic Disorders
- Introduction
- Key Player: Histamine
- H1-Antihistamines
- Histamine Release Inhibitors (Mast-Cell Stabilizers)
- Acknowledgment
- Section 6 Drugs Impacting Ocular, Nasal, and Pulmonary Systems
- Chapter 30 Drugs Used to Treat Ocular and Nasal Disorders
- Introduction
- Therapeutic Classes of Drugs Used to Treat Nasal and Ocular Congestion
- Chapter 31 Drugs Used to Treat Pulmonary Disorders
- Introduction
- Medicinal chemistry of inhaled agents
- Asthma
- Therapeutic Approaches to the Treatment and Management of Asthma
- Therapeutic Classes of Drugs Used to Treat Asthma and Chronic Obstructive Pulmonary Disease
- Chronic Obstructive Pulmonary Disease
- Smoking Cessation
- Cystic Fibrosis
- Idiopathic Pulmonary Fibrosis
- Pulmonary Arterial Hypertension
- Acknowledgements
- Section 7 Drugs Impacting Infectious and Neoplastic Disease Processes
- Chapter 32 Drugs Used to Treat Bacterial Infections
- Introduction
- History
- Antibacterial Nomenclature
- Bacterial Pathogen Identification
- Antibacterial Susceptibility Testing
- Bacterial Resistance and Tolerance
- Therapeutic Considerations
- Mechanistic Classes
- Acknowledgments
- Chapter 33 Drugs Used to Treat Viral Infections
- Introduction
- Virus Structure and Classification
- Infectious Cycle
- Viral Pathogenesis
- General Concepts in the Development of Antiviral Drugs
- Herpesviruses
- Antiviral Drugs to Treat Herpes Viral Infections
- Antiviral Drugs to Treat Cytomegalovirus Infections
- Influenza Viruses
- Antiviral Drugs to Treat Influenza Infections
- Coronaviruses
- Antiviral Drugs to Treat COVID-19
- Respiratory Syncytial Virus
- Antiviral Drugs to Treat Respiratory Syncytial Virus Infections
- Hepatitis
- Antiviral Drugs to Treat Hepatitis B Viral Infections
- Antiviral Drugs to Treat Hepatitis C Viral Infections
- Human Immunodeficiency Virus
- Antiviral Drugs to Treat Human Immunodeficiency Virus Infections
- Rare Viral Diseases
- Antiviral Drugs to Treat Rare Viral Infections
- Chapter 34 Drugs Used to Treat Fungal Infections
- Introduction
- Epidemiology and Economic Impact of Fungal Infections
- Fungal Diseases
- Biochemical Targets of Antifungal Chemotherapy
- Acknowledgment
- Chapter 35 Drugs Used to Treat Parasitic Infections
- Introduction
- Protozoal Infections
- Helminth Infections
- Ectoparasitic infections
- Acknowledgment
- Chapter 36 Drugs Used to Treat Neoplastic Diseases—Classical Chemotherapy
- Cancer
- Therapeutic Classes of Anticancer Drugs
- Chapter 37 Drugs Used to Treat Neoplastic Diseases: Targeted Therapy
- Contemporary Directions and Developments in Cancer Therapy
- Precision Oncology
- Carcinogenesis and Oncogenic Drivers
- Targeted Therapies and Cancer Immunotherapies
- Drug Classes Based on Dysfunctional Pathways and Molecular Targets
- Summary
- Section 8 Therapeutic Biologics
- Chapter 38 Biologics Used in the Treatment of Disease
- Introduction
- Therapeutic Peptide and Protein Drugs
- Antisense Oligonucleotides
- Small Interfering RNAs
- Summary
- Appendix A Predicted pKa and cLog P Values of Commonly Prescribed Drugs
- Appendix B pH Values of Biologic Fluids
- Subject Index
- Drug Index
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