Medicinal Chemistry and Drug Development

1st Edition - February 5, 2025
Imprint: Elsevier
Editor: Gang Liu
Language: English
Paperback ISBN:
9 7 8 - 0 - 4 4 3 - 2 7 4 0 2 - 2
eBook ISBN:
9 7 8 - 0 - 4 4 3 - 2 7 4 0 3 - 9

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… Read more

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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.

Title of Book
Cover image
Title page
Table of Contents
Copyright
List of contributors
About the editor
Preface
Introduction
Chapter 1. Medicinal chemistry and process development of the type 2 diabetes drug sitagliptin
Abstract
Chapter outline
1.1 Introduction to the type 2 diabetes drug sitagliptin
1.2 Incretin and its degrading enzyme dipeptidyl peptidase-4
1.3 Property-based drug design
1.4 Common factors influencing the ADME/T properties of drugs
1.5 Early pharmacological and toxicological studies of dipeptidyl peptidase IV inhibitors
1.6 Confirmation of lead compounds
1.7 Optimization of the β-amino acid series lead compounds
1.8 Clinical studies of the new drug sitagliptin
1.9 Process chemistry of sitagliptin
References
Further reading
Chapter 2. The developmental history of insulin pharmaceuticals
Abstract
Chapter outline
2.1 Introduction to diabetes and insulin
2.2 Development of insulin pharmaceuticals
2.3 Summary and outlook
References
Chapter 3. The developmental trajectory of GLP-1 receptor agonists
Abstract
Chapter outline
3.1 Glucagon-like peptide-1 (GLP-1)
3.2 The development of GLP-1 therapeutics
3.3 The unsuccessful case in GLP-1 drug R&D and the implications and lessons
3.4 Summary and outlook
References
Chapter 4. Antidiabetic drugs based on sodium-glucose cotransporter 2 inhibitors
Abstract
Chapter outline
4.1 Overview of diabetes mellitus and antidiabetic drugs
4.2 Sodium-glucose cotransporter 2 (SGLT2) inhibitors as anti-diabetic drugs
4.3 Successful experience in the development of dapagliflozin
References
Chapter 5. Cholesterol-lowering drug atorvastatin
Abstract
Chapter outline
5.1 Hypercholesterolemia and cardiovascular diseases
5.2 Atorvastatin, the cholesterol-lowering drug
5.3 Medicinal chemistry of atorvastatin
5.4 Summary and outlook
References
Chapter 6. Angiotensin II receptor antagonists for treatment of hypertension: the discovery of losartan and its analogs
Abstract
Chapter outline
6.1 Brief introduction of hypertension and commonly used medications for the treatment of hypertension
6.2 The renin-angiotensin system
6.3 Angiotensin II receptor antagonists
6.4 Discovery of losartan
6.5 Discovery of losartan analogs
References
Chapter 7. Antithrombotic drug—apixaban
Abstract
Chapter outline
7.1 What is thrombosis?
7.2 Treatment of thrombosis
7.3 The medicinal chemistry of apixaban
7.4 Clinical indications of apixaban
7.5 Postclass requirements and references
References
Chapter 8. Development of the anticoagulant drug fondaparinux sodium
Abstract
Chapter outline
8.1 Thrombotic disorders
8.2 Treatment of thrombotic disorders
8.3 Discovery and history of anticoagulant drug: fondaparinux sodium
8.4 Chemical process of fondaparinux sodium
8.5 Summary
References
Chapter 9. Development of the nucleotide antiviral drug sofosbuvir for the hepatitis C virus
Abstract
Chapter outline
9.1 Hepatitis C and hepatitis C virus
9.2 Hepatitis C virus biology
9.3 Discovery of sofosbuvir
9.4 Clinical studies of sofosbuvir
9.5 Summary and outlook
References
Chapter 10. The first HIV-1 integrase inhibitor, raltegravir
Abstract
Chapter outline
10.1 AIDS and HIV
10.2 Anti-HIV drugs
10.3 The discovery journey of raltegravir
10.4 Research on the synthetic process of raltegravir
10.5 Summary and knowledge expansion
References
Chapter 11. Discovery and development of the human immunodeficiency virus protease inhibitor Saquinavir
Abstract
Chapter outline
11.1 Overview of virus
11.2 Human immunodeficiency virus and acquired immunodeficiency syndrome
11.3 HIV protease and inhibitor saquinavir
11.4 Further development of Saquinavir
11.5 Anti-HIV/AIDS drugs and novel treatment strategies
References
Chapter 12. Baloxavir: an antiinfluenza drug with a novel mechanism of action
Abstract
Chapter outline
12.1 Influenza virus
12.2 Antiinfluenza drugs
12.3 Development of baloxavir
References
Chapter 13. Paclitaxel: a natural antitumor agent
Abstract
Chapter outline
13.1 Discovery and development of taxol
13.2 The pharmaceutical chemistry of paclitaxel
13.3 Design strategy for paclitaxel prodrugs
13.4 Summary and outlook
References
Chapter 14. Antitumor drug eribulin
Abstract
Chapter outline
14.1 Introduction
14.2 Antitumor mechanism of eribulin
14.3 The development process of eribulin
14.4 Pharmacological characteristics of eribulin
14.5 Clinical research and safety evaluation of eribulin
14.6 Conclusion
References
Chapter 15. Targeted protein kinase inhibitor imatinib
Abstract
Chapter outline
15.1 Protein kinases (PKs) and protein kinase inhibitors (PKIs) as antineoplastic agents
15.2 Medicinal chemistry of imatinib
15.3 Imatinib resistance and solutions
15.4 Summary
References
Chapter 16. A case study of the irreversible covalent epidermal growth factor receptor (EGFR) inhibitor—afatinib
Abstract
Chapter outline
16.1 Preface
16.2 Epidermal growth factor receptor and quinazoline-based small molecule inhibitors
16.3 Drug design based on covalent inhibition strategies
16.4 Development of covalent irreversible EGFR inhibitor − afatinib
16.5 Synthesis of afatinib
16.6 Summary and knowledge expansion
References
Chapter 17. Medicinal chemistry and process development of the antibreast cancer drug tamoxifen
Abstract
Chapter outline
17.1 Estrogen receptors and breast cancers
17.2 The medicinal chemistry of the selective estrogen receptor modulator tamoxifen
17.3 Clinical investigations of tamoxifen
17.4 Summary, knowledge expansion, and references
References
Chapter 18. Triazole antifungal drug—fluconazole
Abstract
Chapter outline
18.1 Overview of fungal infections
18.2 Overview of antifungal drugs
18.3 The developmental history of fluconazole
18.4 Structure optimization of fluconazole: development of new generation triazole antifungal drugs
References
Chapter 19. Discovery of the antibacterial drug Linezolid and its synthetic technology research
Abstract
Chapter outline
19.1 Development of antibacterial agents
19.2 Discovery of the antibacterial drug Linezolid
19.3 Bioactivity and pharmacokinetics of antibacterial drug Linezolid
19.4 The antibacterial mechanisms of Linezolid
19.5 Study on structure-activity relationship of oxazolidinone antibiotics
19.6 Research on the synthesis process of Linezolid
19.7 Conclusion
References
Further reading
Chapter 20. Carbapenem antibiotic meropenem
Abstract
Chapter outline
20.1 Introduction
20.2 Bacterial resistance and special use level antibacterial drugs
20.3 Case of meropenem
20.4 The progress on other carbapenem antibiotics
References
Chapter 21. Antiparasitic drug praziquantel
Abstract
Chapter outline
21.1 Parasitic diseases
21.2 Antiparasitic drug praziquantel
21.3 Medicinal chemistry of praziquantel
21.4 Green process for praziquantel and its levoisomer
21.5 Green chemistry future
References
Chapter 22. A case study on the proton pump inhibitor omeprazole
Abstract
Chapter outline
22.1 Peptic ulcer
22.2 Why is omeprazole
22.3 Medicinal chemistry of omeprazole
22.4 Clinical applications of omeprazole
22.5 Summary and knowledge expansion
References
Chapter 23. The inhibitors of phosphodiesterase type 5A effectively treat erectile dysfunction
Abstract
Chapter outline
23.1 The nitric oxide-cyclic guanosine monophosphate signaling pathway associated with penile erectile function
23.2 Sildenafil for the management of male erectile dysfunction
23.3 The approval of second and third-generation highly selective phosphodiesterase type 5A inhibitors
23.4 Synthesis of selective phosphodiesterase type 5A inhibitors
23.5 Molecular mechanisms of phosphodiesterase type 5A inhibitors
23.6 Summary and prospect
References
Chapter 24. GABAA receptor agonists: discovery of the general anesthetic propofol and its analogs
Abstract
Chapter outline
24.1 Introduction to anesthesia
24.2 Common drugs in clinical anesthesia
24.3 Medicinal chemistry of the general intravenous anesthetic propofol and its analogs
References
Chapter 25. The discovery of risperidone: a case of multiple target antipsychotic drug
Abstract
Chapter outline
25.1 Antipsychotic drugs
25.2 Medicinal chemistry of risperidone
25.3 Characteristics of risperidone’s effects
References
Chapter 26. A case study on the first-in-class antirenal anemia drug roxadustat
Abstract
Chapter outline
26.1 Renal anemia and its pathogenesis
26.2 Medications for the treatment of renal anemia
26.3 Development process of roxadustat
26.4 Conclusion
References
Chapter 27. Function, pharmaceutical, and pharmacological research and development of natural tetracyclic dipyranocoumarin (+)-calanolide A and its analogs
Abstract
Chapter outline
27.1 Discovery and structural diversity of natural tetracyclic dipyranocoumarins
27.2 Natural nonnucleoside reverse transcriptase inhibitors
27.3 Anti-HIV-1 activity of improved calanolides
27.4 (+)-Calanolide A and its derivatives inhibit replicating and non-replicating Mycobacterium tuberculosis
27.5 Fluorescent activity of nitrofuran derivatives: a revelatory outcome
27.6 Summary and outlook
References
Further reading
Chapter 28. Bisphosphonates: a targeted therapeutic medication for skeletal system
Abstract
Chapter outline
28.1 Unveiling the saga of bisphosphonates
28.2 Elucidating the mechanisms of action of bisphosphonate drugs
28.3 Medicinal chemistry of nitrogen-containing bisphosphonates
28.4 Novel applications of bisphosphonate inhibitors
References
Chapter 29. Celecoxib targets cyclooxygenase in nonsteroidal antiinflammatory drugs
Abstract
Chapter outline
29.1 Nonsteroidal antiinflammatory drugs and cyclooxygenase
29.2 Selective cyclooxygenase-2 inhibitor celecoxib
29.3 Other representative coxib drugs
29.4 Summary and perspective
References
Chapter 30. Case study of antisense oligonucleotides for duchenne muscular dystrophy
Abstract
Chapter outline
30.1 Introduction
30.2 Duchenne muscular dystrophy
30.3 Mechanism of action of antisense oligonucleotide drugs
30.4 The developmental trajectory of antisense oligonucleotide therapeutics targeting the DMD gene
30.5 Summary and outlook
References
Index

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