Modern Drug Synthesis [Hardcover]

Following Contemporary Drug Synthesis and The Art of Drug Synthesis (Wiley, 2004 and 2007), two well-received works, is this new book that 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 (some chapter authors are the actual inventor of the drug) of twenty different drug molecules.Preface xi

Contributors xiii

I. Infectious Diseases 1

Chapter 1. Raltegravir (Isentress), The First-in-class HIV-1 Integrase Inhibitor 3
Julianne A. Hunt

1.1 Background 3

1.2 Pharmacology 5

1.3 Structure-Activity Relationship (SAR) 6

1.4 Pharmacokinetics and Drug Metabolism 8

1.5 Efficacy and Safety 9

1.6 Syntheses 10

1.7 References 13

Chapter 2. Maraviroc (Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV 17
David Price

2.1 Background 17

2.2 Structure-Activity Relationship (SAR) 19

2.3 Pharmacokinetics and Safety 21

2.4 Syntheses 22

2.5 References 27

Chapter 3. Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV 29
Arun K. Ghosh and Cuthbert D. Martyr

3.1 Background 29

3.2 Pharmacology 32

3.3 Structure-Activity Relationship (SAR) 32

3.4 Pharmacokinetics and lÓO