Fused Pyrimidine-Based Drug Discovery

1st Edition - October 8, 2022
Imprint: Elsevier
Editor: Raj Kumar
Language: English
Paperback ISBN:
9 7 8 - 0 - 4 4 3 - 1 8 6 1 6 - 5
eBook ISBN:
9 7 8 - 0 - 4 4 3 - 1 8 6 1 7 - 2

Fused Pyrimidine-Based Drug Discovery covers all categories of fused-pyrimidines along with pharmacological and in silico studies. It covers the chemistry and biological activi… Read more

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Fused Pyrimidine-Based Drug Discovery covers all categories of fused-pyrimidines along with pharmacological and in silico studies. It covers the chemistry and biological activities, as well as the design of novel fused-pyrimidine scaffolds. N-Heterocyclic scaffolds are found in most known drug candidates, and are of interest to medicinal and organic chemists to design, synthesize and evaluate their biological properties. A variety of fused-pyrimidine molecules have been synthesized and extracted from natural resources, and are found to exhibit various biological activities such as antifolates, anticancer agents, analgesics, antimetabolites, CNS active agents and many more. Some of these scaffolds like purines are also known to have involvement in biological processes and are part of the framework of genetic material. This book focuses on the classification, structural chemistry, and chemical and physical properties along with various approaches for their synthesis. This book is ideal for researchers in organic chemistry both in academic and industrial settings, postgraduates in chemistry and medicinal chemistry.

Cover image
Title page
Table of Contents
Copyright
Contributors
Biographies
Foreword
Foreword
Foreword
Acknowledgments
Chapter 1. Introduction
1.1. Introduction
Chapter 2. FDA approved fused pyrimidine-based drugs
2.1. Introduction
2.2. Fused pyrimidine-based anticancer drugs
2.3. Fused pyrimidine-based drugs as anti-viral agents
2.4. Fused pyrimidine-based drugs for cardiovascular disorders
2.5. Fused pyrimidine-based drugs for respiratory disorders
2.6. Fused pyrimidine-based drugs for inflammatory diseases
2.7. Fused pyrimidine-based drugs for neurological disorders
2.8. Fused pyrimidine-based drugs for treatment of benign prostatic hypertrophy (BPH)
2.9. Fused pyrimidine-based drugs for treatment of erectile dysfunction
2.10. Fused pyrimidine-based drugs for miscellaneous use
2.11. Analysis of the approved drugs
Chapter 3. Naturally occurring fused pyrimidine derivatives and their medicinal attributes
3.1. Introduction
Chapter 4. Five-membered ring fused pyrimidine-based derivatives and their biological properties
4.1. Introduction
4.2. Pyrazolo[3,4-d]pyrimidine
4.3. Pyrrolo[1,2-c]pyrimidines, pyrrolo[2,3-d]pyrimidines and pyrrolo[3,2-d]pyrimidines
4.4. Thieno[2,3-d]pyrimidines and thieno[3,2-d]pyrimidines
4.5. Furo[3,2-d]pyrimidines and related heterocycles
4.6. Triazolo[1,5-a]pyrimidines, pyrazolo[1,5-a]pyrimidines, and pyrimido[1,2-a]benzimidazoles
4.7. Pyrazolothienopyrimidine
4.8. Thiazolo[3,2-a]pyrimidines
4.9. Thiazolo[4,5-d]pyrimidines
4.10. Pyrido[4',3':4,5]thieno[2,3-d]pyrimidines
4.11. Recent patents
Chapter 5. FDA approved five-membered ring fused pyrimidine-based derivatives and their biological properties
5.1. Sildenafil
5.2. Valganciclovir
5.3. Duvelisib
5.4. Vidarabine
5.5. Abacavir
5.6. Entecavir
5.7. Ganciclovir
5.8. Acyclovir
5.9. Theophylline
5.10. Pemetrexed
5.11. Zanubrutinib
5.12. Cangrelor
5.13. Ticagrelor
5.14. Fludarabine
5.15. Valaciclovir
5.16. Nelarabine
5.17. Cladribine
5.18. Istradefylline
5.19. Penciclovir
5.20. Tofacitinib
5.21. Ribociclib
5.22. Tenofovir alafenamide
5.23. Ibrutinib
5.24. Udenafil
5.25. Allopurinol
5.26. Ruxolitinib
5.27. Baricitinib
5.28. Zaleplon
5.29. Azathioprine
5.30. Thioguanine
5.31. Anagliptin
5.32. Regadenoson
5.33. Adefovir dipivoxil
5.34. Clofarabine
5.35. Idelalisib
5.36. Didanosine
5.37. Famciclovir
5.38. Dyphylline
5.39. Pentoxifylline
5.40. Caffeine
5.41. Enprofylline
Chapter 6. Benzene fused pyrimidine-based derivatives and their biological properties
6.1. Preface
6.2. Zorifertinib (AZD3759)
6.3. CZh226
6.4. 2-amino-4-methylquinazoline derivatives
6.5. (S)-3-((2-amino-8-fluoroquinazolin-4-yl)amino)hexan-1-ol
6.6. 7-methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one
6.7. BMS-919373
6.8. 1-(4-((3-Chlorophenyl)amino)quinazolin-6-yl)-3-(3,5- difluorophenyl)thiourea
6.9. N-(4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)- phenyl)-2-(pyridin-4-yl)quinazolin-4-amine
6.10. GSK2983559
Chapter 7. Six-membered ring (with N, O or S) fused pyrimidine-based derivatives and biological properties
7.1. Introduction
7.2. Classification
Chapter 8. FDA approved six-membered ring fused pyrimidine-based derivatives
8.1. Methotrexate
8.2. Risperidone
8.3. Pemirolast
8.4. Pralatrexate
8.5. Trametinib
8.6. Triamterene
8.7. Palbociclib
8.8. Dipyridamole
8.9. Prazosin
8.10. Alfuzosin
8.11. Trimetrexate
8.12. Anagrelide
8.13. Quinethazone
8.14. Copanlisib
8.15. Terazosin
8.16. Doxazosin
8.17. Gefitinib
8.18. Erlotinib
8.19. Afatinib
8.20. Dacomitinib
8.21. Vandetanib
8.22. Lapatinib
8.23. Idelalisib
8.24. Raltitrexed
8.25. Asasantin
Chapter 9. Seven-membered ring fused pyrimidine-based derivatives and their biological properties
9.1. Introduction
9.2. Pyrimidine fused with a seven-membered ring containing nitrogen
9.3. Pyrimidine fused with a seven-membered ring containing oxygen
9.4. Pyrimidine fused with a seven-membered ring containing nitrogen and oxygen
9.5. Pyrimidine fused with a seven-membered ring containing sulphur
9.6. Pyrimidine fused with a seven-membered ring containing nitrogen and sulfur
Chapter 10. Eight-membered fused pyrimidine derivatives and their biological properties
10.1. Introduction
10.2. Exploring the reported literature on eight-membered heterocycles fused with a pyrimidine ring
10.3. Tricyclic pyrimidine-fused eight-membered diazocines
10.4. Conclusion
Chapter 11. Molecular modeling studies of fused pyrimidine derivatives at various receptors
11.1. Abacavir
11.2. Acyclovir
11.3. Adefovir dipivoxil
11.4. Allopurinol
11.5. Anagliptin
11.6. Azathioprine
11.7. Baricitinib
11.8. Caffeine
11.9. Cangrelor
11.10. Cladribine
11.11. Clofarabine
11.12. Didanosine
11.13. Dipyridamole
11.14. Duvelisib
11.15. Dyphylline
11.16. Enprofylline
11.17. Entecavir
11.18. Fludarabine
11.19. Ganciclovir
11.20. Ibrutinib
11.21. Idelalisib
11.22. Istradefylline
11.23. Methotrexate
11.24. Nelarabine
11.25. Palbociclib
11.26. Pemetrexed
11.27. PEMIROLAST
11.28. Penciclovir
11.29. Pentoxifylline
11.30. Pralatrexate
11.31. Regadenoson
11.32. Ribociclib
11.33. Risperidone
11.34. Ruxolitinib
11.35. Sildenafil
11.36. Tenofovir alafenamide
11.37. Theophylline
11.38. Ticagrelor
11.39. Thioguanine
11.40. Tofacitinib
11.41. Trametinib
11.42. Triamterene
11.43. Udenafil
11.44. Vidarabine
11.45. Zaleplon
11.46. Zanubrutinib
Index

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Fused Pyrimidine-Based Drug Discovery

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