Medicinal Chemistry and Drug Development describes the key events and roles of medicinal chemistry in the discovery and development of lead compounds into drugs, including target identification, which is accomplished by using 30 case studies. This book outlines all the stages of drug development, including the discovery of active compounds, research on the pharmacological
properties of molecules, and confirmation of drug targets. The role of the case studies is to show the common factors in the successful development of drugs, thereby showing medicinal chemists how best to explore the scientific pathways when developing new drugs. This makes the book especially relevant for senior university students majoring in pharmaceutical sciences as well as graduate students and researchers.
1. Introduction - p. xxi 2. Chapter 1. Medicinal chemistry and process development of the type 2 diabetes drug sitagliptin - p. 1 3. Chapter 2. The developmental history of insulin pharmaceuticals - p. 21 4. Chapter 3. The developmental trajectory of GLP-1 receptor agonists - p. 41 5. Chapter 4. Antidiabetic drugs based on sodium-glucose cotransporter 2 inhibitors - p. 55 6. Chapter 5. Cholesterol-lowering drug atorvastatin - p. 71 7. Chapter 6. Angiotensin II receptor antagonists for treatment of hypertension: the discovery of losartan and its analogs - p. 109 8. Chapter 7. Antithrombotic drug—apixaban - p. 141 9. Chapter 8. Development of the anticoagulant drug fondaparinux sodium - p. 161 10. Chapter 9. Development of the nucleotide antiviral drug sofosbuvir for the hepatitis C virus - p. 185 11. Chapter 10. The first HIV-1 integrase inhibitor, raltegravir - p. 211 12. Chapter 11. Discovery and development of the human immunodeficiency virus protease inhibitor Saquinavir - p. 245 13. Chapter 12. Baloxavir: an antiinfluenza drug with a novel mechanism of action - p. 265 14. Chapter 13. Paclitaxel: a natural antitumor agent - p. 287 15. Chapter 14. Antitumor drug eribulin - p. 327 16. Chapter 15. Targeted protein kinase inhibitor imatinib - p. 349 17. Chapter 16. A case study of the irreversible covalent epidermal growth factor receptor (EGFR) inhibitor—afatinib - p. 387 18. Chapter 17. Medicinal chemistry and process development of the antibreast cancer drug tamoxifen - p. 419 19. Chapter 18. Triazole antifungal drug—fluconazole - p. 449 20. Chapter 19. Discovery of the antibacterial drug Linezolid and its synthetic technology research - p. 465 21. Chapter 20. Carbapenem antibiotic meropenem - p. 489 22. Chapter 21. Antiparasitic drug praziquantel - p. 509 23. Chapter 22. A case study on the proton pump inhibitor omeprazole - p. 531 24. Chapter 23. The inhibitors of phosphodiesterase type 5A effectively treat erectile dysfunction - p. 557 25. GABAA receptor agonists: discovery of the general anesthetic propofol and its analogs - p. 585 26. Chapter 25. The discovery of risperidone: a case of multiple target antipsychotic drug - p. 619 27. Chapter 26. A case study on the first-in-class antirenal anemia drug roxadustat - p. 633 28. Chapter 27. Function, pharmaceutical, and pharmacological research and development of natural tetracyclic dipyranocoumarin (+)-calanolide A and its analogs - p. 651 29. Chapter 28. Bisphosphonates: a targeted therapeutic medication for skeletal system - p. 689 30. Chapter 29. Celecoxib targets cyclooxygenase in nonsteroidal antiinflammatory drugs - p. 711 31. Chapter 30. Case study of antisense oligonucleotides for duchenne muscular dystrophy - p. 735 32. Index - p. 755
Medicinal Chemistry and Drug Development describes the key events and roles of medicinal chemistry in the discovery and development of lead compounds into drugs, including target identification, which is accomplished by using 30 case studies. This book outlines all the stages of drug development, including the discovery of active compounds, research on the pharmacological
properties of molecules, and confirmation of drug targets. The role of the case studies is to show the common factors in the successful development of drugs, thereby showing medicinal chemists how best to explore the scientific pathways when developing new drugs. This makes the book especially relevant for senior university students majoring in pharmaceutical sciences as well as graduate students and researchers.
1. Introduction - p. xxi 2. Chapter 1. Medicinal chemistry and process development of the type 2 diabetes drug sitagliptin - p. 1 3. Chapter 2. The developmental history of insulin pharmaceuticals - p. 21 4. Chapter 3. The developmental trajectory of GLP-1 receptor agonists - p. 41 5. Chapter 4. Antidiabetic drugs based on sodium-glucose cotransporter 2 inhibitors - p. 55 6. Chapter 5. Cholesterol-lowering drug atorvastatin - p. 71 7. Chapter 6. Angiotensin II receptor antagonists for treatment of hypertension: the discovery of losartan and its analogs - p. 109 8. Chapter 7. Antithrombotic drug—apixaban - p. 141 9. Chapter 8. Development of the anticoagulant drug fondaparinux sodium - p. 161 10. Chapter 9. Development of the nucleotide antiviral drug sofosbuvir for the hepatitis C virus - p. 185 11. Chapter 10. The first HIV-1 integrase inhibitor, raltegravir - p. 211 12. Chapter 11. Discovery and development of the human immunodeficiency virus protease inhibitor Saquinavir - p. 245 13. Chapter 12. Baloxavir: an antiinfluenza drug with a novel mechanism of action - p. 265 14. Chapter 13. Paclitaxel: a natural antitumor agent - p. 287 15. Chapter 14. Antitumor drug eribulin - p. 327 16. Chapter 15. Targeted protein kinase inhibitor imatinib - p. 349 17. Chapter 16. A case study of the irreversible covalent epidermal growth factor receptor (EGFR) inhibitor—afatinib - p. 387 18. Chapter 17. Medicinal chemistry and process development of the antibreast cancer drug tamoxifen - p. 419 19. Chapter 18. Triazole antifungal drug—fluconazole - p. 449 20. Chapter 19. Discovery of the antibacterial drug Linezolid and its synthetic technology research - p. 465 21. Chapter 20. Carbapenem antibiotic meropenem - p. 489 22. Chapter 21. Antiparasitic drug praziquantel - p. 509 23. Chapter 22. A case study on the proton pump inhibitor omeprazole - p. 531 24. Chapter 23. The inhibitors of phosphodiesterase type 5A effectively treat erectile dysfunction - p. 557 25. GABAA receptor agonists: discovery of the general anesthetic propofol and its analogs - p. 585 26. Chapter 25. The discovery of risperidone: a case of multiple target antipsychotic drug - p. 619 27. Chapter 26. A case study on the first-in-class antirenal anemia drug roxadustat - p. 633 28. Chapter 27. Function, pharmaceutical, and pharmacological research and development of natural tetracyclic dipyranocoumarin (+)-calanolide A and its analogs - p. 651 29. Chapter 28. Bisphosphonates: a targeted therapeutic medication for skeletal system - p. 689 30. Chapter 29. Celecoxib targets cyclooxygenase in nonsteroidal antiinflammatory drugs - p. 711 31. Chapter 30. Case study of antisense oligonucleotides for duchenne muscular dystrophy - p. 735 32. Index - p. 755
