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Pyrazolo Pyrimides-Based Drug Discovery
1st Edition - April 1, 2023
Author: Rajshekhar Karpoormath
Paperback ISBN:
9 7 8 - 0 - 1 2 - 8 2 3 8 8 7 - 5
eBook ISBN:
9 7 8 - 0 - 1 2 - 8 2 4 2 0 4 - 9
Pyrazolo Pyrimides-Based Drug Discovery describes the medicinal attributes of all isomeric forms of pyrazolopyrimidines with special emphasis on their structure activity… Read more
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Pyrazolo Pyrimides-Based Drug Discovery describes the medicinal attributes of all isomeric forms of pyrazolopyrimidines with special emphasis on their structure activity relationship (SAR). Pyrazolopyrimidines play an important role in organic and medicinal chemistry as they act as a bridge between life sciences and biochemical investigations. Pyrazolopyrimidines are essential scaffolds for generating a wide range of chemical libraries and drug-like candidates to obtain desired therapeutic and pharmacological activity. Specific functional groups are covered, as well as synthesis of bioactive compounds against a specific pathological condition. Isomeric forms of pyrazolo pyrimidine including pyrazolo[5,1-b]pyrimidines, pyrazolo[5,1-a]pyrimidines, pyrazolo[4,3-d]pyrimidines, pyrazolo[1,5-c]pyrimidines and pyrazolo[3,4-d]pyrimidines are discussed, and the discovery of pyrazolopyrimidine-based drug candidates is facilitated by coverage of essential information on functionalization and its effects. This book is ideal for researchers working in organic and medicinal chemistry both in academia and industry.
- Discusses five isomeric forms of pyrazolo pyrimmidines namely pyrazolo[5,1-b]pyrimidines, pyrazolo[5,1-a]pyrimidines, pyrazolo[4,3-d]pyrimidines, pyrazolo[1,5-c]pyrimidines and pyrazolo[3,4-d]pyrimidines
- Describes the chemical structures of the most active pyrazolo pyrimidine derivatives
- Explains the structure activity relationship studies with respect to each biological activities
- Includes functionalization of various groups on pyrimidine scaffold for designing bio-active molecules
Researchers in organic chemistry both in academic and industrial settings, postgraduates in chemistry and medicinal chemistry, Researchers in pharmaceutical industries, chemical and pesticide industries
1. Title
2. IntroductionHistory and BackgroundPyrazolo pyrimidine isomers and TautomerismPyrazolo pyrimidine containing marketed drugs and biological activityPhysical properties: Aromaticity, UV, IR, NMR, X-Ray diffractionChemical Properties: Reactions with electrophiles, nucleophiles, ring opening and closing and rearrangement reactions
3. Synthetic strategiesSynthesis of Pyrazolo(1,5-a)pyrimidineSynthesis of Pyrazolo(3,4-d)pyrimidineSynthesis of Pyrazolo(4,3-d)pyrimidineSynthesis of Pyrazolo(1,5-c)pyrimidine
4. Activity and SAR studies Pyrazolo(1,5-a)pyrimidine Anti-cancer agents Anti-proliferative CDK inhibitors c-Src, lck and chk inhibitors B-Raf kinase inhibitors Pim kinase inhibitors KDR kinase inhibitors Tyrosine kinase JNK inhibitors JAK1 JH2 pseudokinase and VPS34 Trk kinase inhibitor Central nervous system (CNS) agents Benzodiazepine receptor modulators 5-HT6 receptor antagonists Anti-infectious agents CRF-1 receptor antagonists Miscellaneous agents Pyrazolo(3,4-d)pyrimidine Anti-cancer Lck, Src, Kdr and Tie-2 inhibitors Abl inhibitors Activated Cdc42Hs-associated kinase 1 inhibitors p38α kinase inhibitors Aurora kinases and CDK1 inhibitors 7Akt/p70S6K inhibitors CK 1 inhibitors Antiproliferative agents Proto-oncogene tyrosine-protein kinase Mer inhibitors Topoisomerase II inhibitors Xanthine oxidase inhibitors Antimicrobial activity Antibacterial and antifungal activity Antitubercular activity Antiviral activities Insulin-like growth factor-1 receptor (IGF1R) and ErbB-family receptor kinases Anti-inflammatory activity Pyrazolo(4,3-d)pyrimidine Anti-cancer Anti-infectious Central nervous system (CNS) agents Phosphodiesterase-5 inhibitor Adenosine receptor antagonists Cytokinin activity Miscellaneous agents Pyrazolo(1,5-c)pyrimidine TARP g-8 Selective AMPAR Negative Modulators Miscellaneous agents
5. Classes of Pyrazolopyrimidines-Based Drugs Pyrazolo(1,5-a)pyrimidine-Based Drugs Zaleplon (Sonata) Indiplon Ocinaplon Lorediplon Verucerfont Dinaciclinib Anagliptin Larotrectinib Selitrectinib Pyrazolo(3,4-d)pyrimidine-Based Drugs Allopurinol Ibrutinib Oxypurinol PF-04447943 Sapanisertib Preladenant Parsaclisib Umbralisib Futibatinib Pyrazolo(4,3-d)pyrimidine-Based Drugs Sildinafil Udenafil Gisadenafil Lodenafil carbonate Pyrazolo(1,5-c)pyrimidine-Based Drugs Lead Hits/clinical trials/patents
6. Miscellaneous application Industrial applications such as dyes, paints, agrochemicals etc.
7. Brief discussion on Patents and activities List of published Patents in chronological order covering pyrazolo pyrimidine scaffold with diverse biological activities
8. Conclusion
9. References
- No. of pages: 370
- Language: English
- Edition: 1
- Published: April 1, 2023
- Imprint: Elsevier
- Paperback ISBN: 9780128238875
- eBook ISBN: 9780128242049
RK
Rajshekhar Karpoormath
Rajshekhar Karpoormath’s research group at University of KwaZulu-Natal, South Africa specialises on the synthesis of aza-heterocycles and their pharmacological applications. One such versatile scaffold of our research interest is pyrazolopyrimidines and their broad range of medicinal applications. We have published several review articles on aza-heterocycles and recently published two full review articles in European Journal of Medicinal Chemistry (2017) 126, 298-352 and Bioorganic & Medicinal Chemistry (2018), 26(2), 309-339 on pyrazolo[1,5-a]pyrimidine and pyrazolo[4,3-d]pyrimidine scaffolds respectively. Our exercise of writing the two reviews on pyrazolopyrimidine analogues has given us good understanding and knowledge on this scaffold. In addition we have studied and collected extensive literature on this topic, thus having required credentials and knowledge in writing an extensive book on pyrazolopyrimidine with special emphasis on their medicinal applications and Structure Activity Relationship (SAR) Studies.
Affiliations and expertise
Research Group, University of KwaZulu-Natal, South Africa