Modern Drug Synthesis demystifies the process of modern drug discovery for practitioners and students. An enhanced introduction covers areas such as background, pharmacology, SAR, PK/PD, efficacy, and safety. Focusing on the advantages of process synthesis versus the discovery synthetic route, Modern Drug Synthesis features authoritative coverage by distinguished editors and authors of twenty different drug molecules.

Contents

Part 1: Infectious Diseases

Chapter 1: The First-in-class HIV-1 Integrase Inhibitor

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 2: Maraviroc (Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV

• Background
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Safety
• Syntheses

Chapter 3: Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Part 2: Cancer

Chapter 4: Decitabine (Dacogen), A DNA Methyltransferase Inhibitor for Cancer

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 5: Capecitabine (Xeloda), An Oral Chemotherapy Agent

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Efficacy
• Syntheses

Chapter 6: Sorafenib (Nexavar), A Multi-kinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable Hepatocellular Carcinoma

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 7: Sunitinib (Sutent), An Angiogenesis Inhibitor

• Background
• Discovery and Development
• Syntheses
• Discovery Route
• Process Route

Chapter 8: Bortezomib (Velcade), A First-in-class Proteasome Inhibitor

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 9: Pazopanib (Votrient), A VEGFR Tyrosine Kinase Inhibitor for Cancer

• Background
• Pharmacology
• Structure Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses
• Other VEGFR Inhibitors in Development: Vandetanib and Cediranib

Part 3: Cardiovascular and Metabolic Diseases

Chapter 10: Sitagliptin (Januvia), A Treatment for Type 2 Diabetes

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 11: Aliskiren (Tekturna), The First-in-class Renin Inhibitor for Hypertension

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 12: Vernakalant (Kynapid), An Investigational Drug for the Treatment of Atrial Fibrillation

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 13: Conivaptan (Vaprisol), Vasopressin V1a and V2 Antagonist for Hyponatremia

• Background
• Pharmacology
• Structure-Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 14: Rivaroxaban (Xarelto), A Factor Xa Inhibitor for the Treatment of Thrombotic Events

• Background
• Pharmacology
• Structure Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses
• Compounds in Development: Apixaban and Otamixaban

Chapter 15: Endothelin Antagonists for the Treatment of Pulmonary Arterial Hypertension

• Background
• Treatment of PAH
• Endothelin Antagonists
• Synthesis of Bosentan
• Synthesis of Sitaxsentan
• Synthesis of Ambrisentan
• Conclusion

Part 4: Central Nervous System Diseases

Chapter 16. Varenicline (Chantix), An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation

• Background
• Discovery Chemistry Program
• Pharmacology
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 17: Donepezil, Rivastigmine, Galantamine: Cholinesterase Inhibitors for Alzheimer's Disease

• Background
• Pharmacology
• Structure Activity Relationship (SAR)
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Synthesis of Donepezil
• Synthesis of Rivastigmine
• Synthesis of Galantamine

Chapter 18: Aprepitant (Emend), A NK1 Receptor Antagonist for the Treatment of Post-chemotherapy Emesis

• Background
• In Vitro Pharmacology and Structure-Activity Relationships
• In Vivo Pharmacology
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 19: Armodafinil (Nuvigil), A Psychostimulant for the Treatment of Narcolepsy

• Background
• Pharmacology
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Synthesis

Part 5: Miscellaneous

Chapter 20: Raloxifene (Evista), A Selective Estrogen Receptor Modulator (SERM)

• Background
• Mechanism of Action
• Pharmacokinetics and Drug Metabolism
• Efficacy and Safety
• Syntheses

Chapter 21: A Prostanoid FP Agonist for Glaucoma

• Background
• Syntheses

Index

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