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Summary

The all-inclusive book on the cutting-edge science driving the medicinal chemistry of the latest drugs

The successor to the editors' two highly acclaimed works on drug synthesis, Contemporary Drug Synthesis and The Art of Drug Synthesis, this book provides refocused and extensive new coverage detailing how chemistry, biology, and pharmacokinetics integrate to spearhead successful medical findings. Modern Drug Synthesis carries on the mission of delivering the most up-to-date developments unfolding in this rapidly evolving field by placing a stronger emphasis on medicinal chemistry and pharmacology, in addition to drug synthesis. Other highlights include: *

Chapters are logically divided into categories such as background of disease area, pharmacology, SAR (structure-activity relationships), pharmacokinetics and drug metabolism, efficacy and safety, and synthesis *

Expert analysis of the pros and cons of different synthetic routes *

A step-by-step breakdown of today's drug discovery process for professionals and students *

Supporting case studies in each chapter

Modern Drug Synthesis shows that whether drug synthesis is in early development or the process stage, the ability to design elegant and economical synthetic routes is often a major factor making a drug a commercial winner. Easy to follow and stacked with valuable information on the present and future direction of medicinal chemistry, Modern Drug Synthesis is the one guide that paints a clear and complete picture of this complex subject.

Table of Contents

Preface
Contributors
Infectious Diseases
Raltegravir (Isentress), The First-in-class HIV-1 Integrase Inhibitor
Background
Pharmacology
Structure-Activity Relationship (SAR)
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Syntheses
References
Maraviroc (Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV
Background
Structure-Activity Relationship (SAR)
Pharmacokinetics and Safety
Syntheses
References
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
References
Cancer
Decitabine (Dacogen), A DNA Methyltransferase Inhibitor for Cancer
Background
Pharmacology
Structure-Activity Relationship (SAR)
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Syntheses
References
Capecitabine (Xeloda), An Oral Chemotherapy Agent
Background
Pharmacology
Structure-Activity Relationship (SAR)
Pharmacokinetics and Efficacy
Syntheses
References
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
References
Sunitinib (Sutent), An Angiogenesis Inhibitor
Background
Discovery and Development
Syntheses
Discovery Route
Process Route
References
Bortezomib (Velcade), A First-in-class Proteasome Inhibitor
Background
Pharmacology
Structure-Activity Relationship (SAR)
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Syntheses
References
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
References
Cardiovascular and Metabolic Diseases
Sitagliptin (Januvia), A Treatment for Type 2 Diabetes
Background
Pharmacology
Structure-Activity Relationship (SAR)
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Syntheses
References
Aliskiren (Tekturna), The First-in-class Renin Inhibitor for Hypertension
Background
Pharmacology
Structure-Activity Relationship (SAR)
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Syntheses
References
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
References
Conivaptan (Vaprisol), Vasopressin V1a and V2 Antagonist for Hyponatremia
Background
Pharmacology
Structure-Activity Relationship (SAR)
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Syntheses
References
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
References
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
References
Central Nervous System Diseases
Varenicline (Chantix), An ¿4ß2 Nicotinic Receptor Partial Agonist for Smoking Cessation
Background
Discovery Chemistry Program
Pharmacology
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Syntheses
References
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
References
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
References
Armodafinil (Nuvigil), A Psychostimulant for the Treatment of Narcolepsy
Background
Pharmacology
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Synthesis
References
Miscellaneous
Raloxifene (Evista), A Selective Estrogen Receptor Modulator (SERM)
Background
Mechanism of Action
Pharmacokinetics and Drug Metabolism
Efficacy and Safety
Syntheses
References
Latanoprost (Xalatan), A Prostanoid FP Agonist for Glaucoma
Background
Syntheses
References
Index
Table of Contents provided by Publisher. All Rights Reserved.

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