
Privileged Scaffolds in Drug Discovery
- 1st Edition - July 19, 2023
- Imprint: Academic Press
- Editors: Bin Yu, Ning Li, Caiyun Fu
- Language: English
- Paperback ISBN:9 7 8 - 0 - 4 4 3 - 1 8 6 1 1 - 0
- eBook ISBN:9 7 8 - 0 - 4 4 3 - 1 8 6 1 2 - 7
Privileged Scaffolds in Drug Discovery is the most complete and up-to-date work in the area. Covering a wide range of privileged structures, it is a perfect reference for scien… Read more

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Request a sales quotePrivileged Scaffolds in Drug Discovery is the most complete and up-to-date work in the area. Covering a wide range of privileged structures, it is a perfect reference for scientists involved in targeted drug development.
The editors recruited experts from several prestigious Chinese institutions to cover the areas of antiviral drugs, chalcone, pyrimidine, (benz)imidazoles, natural product-derived privileged scaffolds, N-Sulfonyl carboxamides, kinase inhibitors, antitumor molecules, antineurodegenerative drugs, triazoles, oxazolidinone, indole and indoline scaffolds, tigliane diterpenoids, peptide and peptide-based drugs, quassinoids, and others including pseudonatural products, macrocycles, stable peptides and peptidomimetics. The book also explores scaffolds in drug molecules approved in recent years.
Privileged Scaffolds in Drug Discovery is a complete reference for researchers in drug discovery and organic synthesis, in academic and corporate settings, who are investigating privileged structures upon which to base new drugs. Researchers in medicinal chemistry and chemical biology will also find the contents of this book valuable.
- Provides wide coverage of privileged scaffolds in new drug discovery
- Includes complex and diverse natural product scaffolds
- Covers applications to peptides and peptide-based drugs
- Cover image
- Title page
- Table of Contents
- Copyright
- List of contributors
- Preface
- Introduction
- Chapter 1. Thiazole, a privileged scaffold in drug discovery
- 1. Introduction
- 2. Thiazole derivatives as therapeutic agents
- 3. Conclusions
- Chapter 2. Chalcones: Diverse biological activities and structure–activity relationships
- 1. Background
- 2. Biological activities of chalcone derivatives
- 3. Conclusion
- Chapter 3. Privileged chalcone scaffolds in drug discovery
- 1. Introduction
- 2. Simple chalcones classified by representative mechanisms of action
- 3. Representative hybrid chalcones
- 4. Conclusions and perspectives
- Chapter 4. The N-sulfonyl carboxamide moiety as a privileged structure in approved drugs
- 1. Introduction
- 2. Physicochemical properties and conformations of N-sulfonyl carboxamides
- 3. Structures and protein targets of marketed drugs 1–27 comprising N-sulfonyl carboxamide moieties
- 4. Perspective
- 5. Conclusion
- Chapter 5. Scaffolds in cytotoxic drugs and novel antitumor molecules interacting with nucleic acids
- 1. DNA intercalators
- 2. Topoisomerase inhibitors
- 3. G-quadruplex ligands
- Chapter 6. Triazoles: a privileged scaffold in drug design and novel drug discovery
- 1. Introduction
- 2. 1,2,3-Triazole as bioisosteres
- 3. Biological significance
- 4. Conclusions and prospects
- Chapter 7. Oxazolidinone scaffolds in drug discovery and development
- 1. Introduction
- 2. Launched oxazolidinone antibacterial drugs
- 3. Modification of linezolid-based oxazolidinone medications
- 4. Other novel oxazolidinone derivatives
- 5. Effects of oxazolidinone derivatives on other diseases
- 6. Summary and perspective
- Chapter 8. Indole and indoline scaffolds in drug discovery
- 1. Background of indole and indoline
- 2. Chemical profile of indole and indoline
- 3. Pharmacologic profile of indole and indoline
- 4. Conclusion and future perspectives
- Chapter 9. Cyanopyridine as a privileged scaffold in drug discovery
- 1. Introduction
- 2. Synthesis of cyanopyridine derivatives
- 3. Conclusion
- Chapter 10. Indazole as a privileged scaffold in drug discovery
- 1. Overview of the indazole
- 2. Synthesis route for indazole derivatives
- 3. Medicinal importance
- 4. Structure–activity relationships
- Chapter 11. (Benz)imidazoles: privileged scaffolds in medicinal chemistry
- 1. Introduction
- 2. (Benz)imidazole-based anticancer agents
- 3. (Benz)imidazole-based antitubercular agents
- 4. (Benz)imidazole-based antibacterial agents
- 5. (Benz)imidazole-based antifungal agents
- 6. (Benz)imidazole-based antiparasitic agents
- 7. (Benz)imidazole-based antiviral agents
- 8. (Benz)imidazole-based antiinflammatory agents
- 9. (Benz)imidazole-based anti-Alzheimer’s disease agents
- 10. (Benz)imidazole-based hypotensive agents
- 11. Conclusion and perspectives
- Chapter 12. Tranylcypromine (TCP): a privileged scaffold for designing histone lysine demethylase 1 inhibitors
- 1. Introduction
- 2. Structure and function of lysine-specific demethylase 1
- 3. Lysine-specific demethylase inhibitors with tranylcypromine privileged scaffold
- 4. Conclusion and perspectives
- Chapter 13. Applications of piperazine scaffold in drug design
- 1. Introduction
- 2. Applications of piperazine scaffold in drug design
- 3. Conclusion
- Chapter 14. Thiols as a privileged scaffold against metallo-β-lactamases
- 1. Introduction
- 2. Thiol-based metallo-β-lactamase inhibitors
- 3. Challenges in thiol-based metallo-β-lactamase inhibitors
- 4. Perspectives
- Chapter 15. Tetrahydro-β-carboline scaffold in drug discovery
- 1. Introduction
- 2. Structures and activities of synthetic tetrahydro-β-carboline derivatives
- Chapter 16. Benzoxaborole: a privileged scaffold for drug discovery
- 1. Introduction
- 2. Benzoxaboroles for antibacterial activity
- 3. Benzoxaboroles for antifungal activity
- 4. Benzoxaboroles for antiviral activity
- 5. Benzoxaboroles for antiinflammatory activity
- 6. Benzoxaboroles for antiprotozoal activity
- 7. Benzoxaboroles for anticancer activity
- 8. Chemical synthesis approaches to benzoxaboroles
- 9. Summary and perspectives
- Chapter 17. Privileged scaffolds in anti-diabetic drug discovery
- 1. Introduction
- 2. Thiazolidinediones
- 3. Biphenyl scaffold
- 4. Spirocycles
- 5. Chalcone scaffold
- 6. Chromone scaffold
- 7. Pyrazolone scaffold
- 8. Benzisoxazole scaffold
- 9. Quinoxalinone scaffold
- 10. Conclusion
- Declaration of competing interest
- Chapter 18. Authentic HIV-1 integrase inhibitors for the treatment of HIV-1/AIDS
- 1. HIV-1/AIDS and its treatment
- 2. HIV-1 integrase and HIV-1 integrase inhibitors
- 3. Approved HIV-1 integrase strand transfer inhibitors
- 4. Development of HIV-1 integrase strand transfer inhibitors
- 5. Pharmacophore and binding modes of HIV-1 integrase strand transfer inhibitors
- 6. HIV-1 integrase allosteric inhibitors
- 7. Conclusions
- Chapter 19. 2-Aminopyrimidine: a privileged scaffold in kinase drug discovery
- 1. Introduction
- 2. Binding modes of 2-anilinopyrimidine–based kinase drugs
- 3. 2-Anilinopyrimidine–based representative kinase drugs
- 4. Conclusions
- Chapter 20. Alzheimer's disease therapeutics: current strategies and future directions
- 1. Introduction
- 2. Established therapeutic targets and therapies for Alzheimer's disease
- 3. Future directions
- 4. Conclusion
- Chapter 21. Sulfonyl fluorides as warheads in drug discovery
- 1. Introduction
- 2. Reactivity of sulfonyl fluorides towards amino acids
- 3. Application of sulfonyl fluoride derivatives in drug discovery
- 4. Conclusion and perspective
- Chapter 22. α,β-Bifunctionalized carbonyl compounds as privileged motifs in drug discovery and their synthetic protocols
- 1. Introduction
- 2. Asymmetric catalytic hydrogenation
- 3. Sharpless asymmetric dihydroxylation and aminohydroxylation
- 4. Asymmetric aldol reaction
- 5. Nucleophilic ring-opening reaction
- 6. Asymmetric Henry reaction
- 7. Asymmetric aza-Henry reaction for synthesis of α,β-biamino carbonyl skeleton
- 8. Asymmetric multicomponent reactions
- 9. Conclusions
- Chapter 23. Diarylpyrimidines and related analogs as antiviral agents
- 1. Introduction
- 2. Diarylpyrimidines and related analogs as anti-human immunodeficiency virus-1 agents
- 3. Anticoronavirus agents
- 4. Discussion and prospects
- Chapter 24. Organic synthetic methodology-based new scaffolds in drug discovery
- 1. Introduction
- 2. Fused heterocyclic scaffolds
- 3. Bridged scaffolds
- 4. Discussion
- Chapter 25. Natural resource of anti–human immunodeficiency virus leading compounds: tigliane diterpenoids
- 1. Introduction
- 2. Distribution
- 3. Tigliane diterpenoids
- 4. Anti–human immunodeficiency virus activities and structure–activity relationships
- 5. Biosynthesis and synthesis
- 6. Drug developments
- 7. Conclusions
- Chapter 26. Biological phenethyl glycosides from plants
- 1. Introduction
- 2. Chemistry of phenethyl glycosides
- 3. Biosynthetic pathway and biotransformation
- 4. Biological activities and mechanisms
- 5. Metabolism and bioavailability
- Chapter 27. Triterpenoids and saponins in drug discovery
- 1. Introduction
- 2. Sources and chemical structures of triterpenoids
- 3. Pharmacologic activities
- 4. Conclusion
- Chapter 28. Casbene-derived diterpenoids
- 1. Introduction
- 2. Tigliane diterpenoids
- 3. Ingenane diterpenoids
- 4. Daphnane-type diterpenoids
- Chapter 29. Quassinoids: phytochemistry and antitumor prospect
- 1. Introduction
- 2. Biosynthetic pathway of quassinoids
- 3. Distribution and classification of quassinoids
- 4. Phytochemical investigations
- 5. Antitumor activities of quassinoids
- 6. Summary and perspectives
- Chapter 30. Structural diversity, biosynthesis, and biological functions of meroterpenoids from microbial metabolites
- 1. Introduction
- 2. Structural diversity and representative compounds of bacterium-derived meroterpenoids
- 3. Structural diversity and representative compounds of fungus-derived meroterpenoids
- 4. Biosynthesis of meroterpenoids from microbial metabolites
- 5. Biological functions of meroterpenoids from microbial metabolites
- Chapter 31. Glucocorticoid compounds in drug discovery by targeting glucocorticoid receptor protein
- 1. A brief history of cortisone discovery
- 2. Glucocorticoids
- 3. Cortisone derivatives
- 4. Outlook
- 5. Conclusions
- Chapter 32. Peptide and peptide-based drugs
- 1. Introduction
- 2. Peptide drugs targeting glucagon-like peptide-1 receptor
- 3. Peptide drugs targeting glucagon-like peptide-2 receptor
- 4. Peptide drugs targeting guanylyl cyclase C receptor
- 5. Peptide drugs targeting calcitonin receptor
- 6. Peptide drugs targeting gonadotropin-releasing hormone receptor
- 7. Peptide drugs targeting active site of 20S proteasome
- 8. Peptide drugs targeting nucleotide-binding oligomerization domain-containing protein 2 protein
- 9. Peptide drugs targeting oxytocin receptor
- 10. Peptide drugs targeting thyrotropin-releasing hormone
- 11. Peptide drugs targeting melanocortin receptors
- 12. Peptide drugs targeting parathyroid hormone 1 receptor
- 13. Peptide drugs targeting guanylate cyclase C
- 14. Peptide drugs targeting NPR-A (natriuretic peptide receptor-A)
- 15. Peptide drugs targeting angiotensin II type 1 receptor
- 16. Peptide drugs targeting β2 receptor
- 17. Peptide drugs targeting glycoprotein 41
- 18. Peptide drugs targeting growth hormone releasing hormone receptor
- 19. Peptide drugs targeting N-type calcium channels
- 20. Peptide drugs targeting thrombopoietin receptor
- 21. Peptide drugs targeting erythropoietin receptor
- 22. Peptide drugs as active principal of pulmonary surfactant
- 23. Peptide drugs targeting calcium-sensing receptor
- 24. Peptide drugs targeting melanocortin 1 receptor
- 25. Peptide drugs targeting SSTRs
- 26. Peptide drugs targeting melanocortin-4 receptor
- 27. Conclusions
- Chapter 33. Stapled peptides for new drug discovery
- 1. Introduction
- 2. Transition metal-catalyzed reaction
- 3. Acid–amine condensation reaction
- 4. Click chemistry
- 5. Photocatalytic reactions
- 6. Other reactions
- 7. Conclusion and outlook
- Chapter 34. Current status and trends in research and development of polypeptide drugs
- 1. Concept
- 2. Synthesis methods
- 3. Purification and application
- 4. The state of polypeptide drug development
- 5. Approved typical peptide drugs
- 6. Prospects
- Chapter 35. Unique opportunities of metal scaffolds in drug design
- 1. Introduction
- 2. Metals as coordinative scaffolds
- 3. Metal complexes as structural scaffolds
- 4. Catalytic metal drugs
- 5. Conclusion
- Chapter 36. N-Heterocyclic carbene as privileged scaffold in medicinal inorganic chemistry
- 1. Introduction
- 2. Platinum N-heterocyclic carbene complexes
- 3. Rhodium N-heterocyclic carbene complexes
- 4. Gold N-heterocyclic carbene complexes
- 5. Silver N-heterocyclic carbene complexes
- 6. Conclusion
- Chapter 37. Selenium-containing heterocycles
- 1. Introduction
- 2. Seleno-heterocycles: selenium in sp3 hybridization
- 3. Seleno-heterocycles: selenium in sp2 hybridization
- 4. Concluding remarks and future perspectives
- Chapter 38. Computational methods for scaffold hopping
- 1. Introduction
- 2. Computational methods of scaffold hopping
- 3. Conclusion
- Index
- Edition: 1
- Published: July 19, 2023
- Imprint: Academic Press
- No. of pages: 986
- Language: English
- Paperback ISBN: 9780443186110
- eBook ISBN: 9780443186127
BY
Bin Yu
NL
Ning Li
CF