UID:
almahu_9949697973102882
Format:
1 online resource (379 pages)
ISBN:
9780443186172
Series Statement:
Heterocyclic Drug Discovery
Content:
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.
Note:
Front Cover -- Fused Pyrimidine-Based Drug Discovery -- Fused Pyrimidine-Based Drug Discovery Heterocyclic Drug Discovery -- Copyright -- Contents -- Contributors -- Biographies -- Foreword -- Foreword -- Foreword -- Acknowledgments -- 1 - Introduction -- 1.1 Introduction -- References -- 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 -- References -- 3 - Naturally occurring fused pyrimidine derivatives and their medicinal attributes -- 3.1 Introduction -- 3.1.1 Fused pyrimidine from plants -- 3.1.2 Fused pyrimidine derivatives from fungi -- 3.1.3 Fused pyrimidine derivatives obtained from sponges -- References -- 4 - Five-membered ring fused pyrimidine-based derivatives and their biological properties -- 4.1 Introduction -- 4.2 Pyrazolo[3,4-d]pyrimidine -- 4.2.1 Anticancer activity -- 4.2.2 α-amylase and α-glucosidase inhibitors -- 4.2.3 Anti-inflammatory activity -- 4.2.4 Antibacterial activity -- 4.3 Pyrrolo[1,2-c]pyrimidines, pyrrolo[2,3-d]pyrimidines and pyrrolo[3,2-d]pyrimidines -- 4.3.1 PI3Kα inhibitors -- 4.3.2 Antitumor agents -- 4.4 Thieno[2,3-d]pyrimidines and thieno[3,2-d]pyrimidines -- 4.4.1 DNase I inhibition activity -- 4.4.2 Anti-proliferative activity -- 4.5 Furo[3,2-d]pyrimidines and related heterocycles.
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4.5.1 G-protein coupled receptor (GPCR)119 agonists -- 4.5.2 Anti-cancer agents -- 4.5.3 Anti-HCV activity -- 4.5.4 Epidermal growth factor receptor (EGFR) inhibitors -- 4.6 Triazolo[1,5-a]pyrimidines, pyrazolo[1,5-a]pyrimidines, and pyrimido[1,2-a]benzimidazoles -- 4.6.1 Anti-cancer activity -- 4.6.2 Antitubercular activity -- 4.7 Pyrazolothienopyrimidine -- 4.8 Thiazolo[3,2-a]pyrimidines -- 4.8.1 Antimicrobial activity -- 4.8.2 Anticancer activity -- 4.8.3 Anti-inflammatory agents -- 4.8.4 Antibacterial and antitubercular agents -- 4.9 Thiazolo[4,5-d]pyrimidines -- 4.9.1 Cyclooxygenase inhibitors -- 4.10 Pyrido[4',3':4,5]thieno[2,3-d]pyrimidines -- 4.11 Recent patents -- Acknowledgments -- References -- 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 -- References -- 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.
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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 -- References -- 7 - Six-membered ring (with N, O or S) fused pyrimidine-based derivatives and biological properties -- 7.1 Introduction -- 7.2 Classification -- 7.2.1 Nitrogen-containing six-membered rings fused with pyrimidine -- 7.2.1.1 Pyrido-pyrimidines -- 7.2.1.1.1 Pyrido[3,4-d]pyrimidines -- 7.2.1.1.2 Pyrido[2,3-d]pyrimidines -- 7.2.1.1.3 Pyrido[3,2-d]pyrimidines -- 7.2.1.1.4 Pyrido[4,3-d] pyrimidines -- 7.2.1.2 Pyrimidopyrimidines -- 7.2.1.2.1 Pyrimidio[1,6-a] and [1,6-c]pyrimidines -- 7.2.1.2.2 Pyrimido[4,5-d]pyrimidines -- 7.2.1.2.3 Pyrimido[5,4-d]Pyrimidines -- 7.2.1.2.4 Pyrimido[1,2-a]pyrimidines -- 7.2.1.3 Pteridine -- 7.2.2 Oxygen-containing six-membered ring fused with pyrimidine -- 7.2.2.1 Chromeno[2,3-d]pyrimidines -- 7.2.2.2 Pyrano[3,2-d]pyrimidines -- 7.2.2.3 Pyrano[2,3-d]pyrimidines -- 7.2.3 Sulphur containing six-membered rings fused with a pyrimidine -- 7.2.3.1 Thiopyrano[3,2-d]pyrimidines -- References -- 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 -- References.
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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 -- References -- 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 -- 10.3.1 Eight-membered rings (azocine) -- 10.4 Conclusion -- References -- 11 - Molecular modeling studies of fused pyrimidine derivatives at various receptors -- 11.1 Abacavir -- 11.1.1 Mechanism of action -- 11.1.2 Binding mode analysis -- 11.2 Acyclovir -- 11.2.1 Mechanism of action -- 11.2.2 Binding mode analysis -- 11.3 Adefovir dipivoxil -- 11.3.1 Mechanism of action -- 11.3.2 Binding mode analysis -- 11.4 Allopurinol -- 11.4.1 Mechanism of action -- 11.4.2 Binding mode analysis -- 11.5 Anagliptin -- 11.5.1 Mechanism of action -- 11.5.2 Binding mode analysis -- 11.6 Azathioprine -- 11.6.1 Mechanism of action -- 11.6.2 Binding mode analysis -- 11.7 Baricitinib -- 11.7.1 Mechanism of action -- 11.7.2 Binding mode analysis -- 11.8 Caffeine -- 11.8.1 Mechanism of action -- 11.8.2 Binding mode analysis -- 11.9 Cangrelor -- 11.9.1 Mechanism of action -- 11.9.2 Binding mode analysis -- 11.10 Cladribine -- 11.10.1 Mechanism of action -- 11.10.2 Binding mode analysis -- 11.11 Clofarabine -- 11.11.1 Mechanism of action -- 11.11.2 Binding mode analysis -- 11.12 Didanosine.
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11.12.1 Mechanism of action -- 11.12.2 Binding mode analysis -- 11.13 Dipyridamole -- 11.13.1 Mechanism of action -- 11.13.2 Binding mode analysis -- 11.14 Duvelisib -- 11.14.1 Mechanism of action -- 11.14.2 Binding mode analysis -- 11.15 Dyphylline -- 11.15.1 Mechanism of action -- 11.15.2 Binding mode analysis -- 11.16 Enprofylline -- 11.16.1 Mechanism of action -- 11.16.2 Binding mode analysis -- 11.17 Entecavir -- 11.17.1 Mechanism of action -- 11.17.2 Binding mode analysis -- 11.18 Fludarabine -- 11.18.1 Mechanism of action -- 11.18.2 Binding mode analysis -- 11.19 Ganciclovir -- 11.19.1 Mechanism of action -- 11.19.2 Binding mode analysis -- 11.20 Ibrutinib -- 11.20.1 Mechanism of action -- 11.20.2 Binding mode analysis -- 11.21 Idelalisib -- 11.21.1 Mechanism of action -- 11.21.2 Binding mode analysis -- 11.22 Istradefylline -- 11.22.1 Mechanism of action -- 11.22.2 Binding mode analysis -- 11.23 Methotrexate -- 11.23.1 Mechanism of action -- 11.23.2 Binding mode analysis -- 11.24 Nelarabine -- 11.24.1 Mechanism of action -- 11.24.2 Binding mode analysis -- 11.25 Palbociclib -- 11.25.1 Mechanism of action -- 11.25.2 Binding mode analysis -- 11.26 Pemetrexed -- 11.26.1 Mechanism of action -- 11.26.2 Binding mode analysis -- 11.27 PEMIROLAST -- 11.27.1 Mechanism of action -- 11.27.2 Binding mode analysis -- 11.28 Penciclovir -- 11.28.1 Mechanism of action -- 11.28.2 Binding mode analysis -- 11.29 Pentoxifylline -- 11.29.1 Mechanism of action -- 11.29.2 Binding mode analysis -- 11.30 Pralatrexate -- 11.30.1 Mechanism of action -- 11.30.2 Binding mode analysis -- 11.31 Regadenoson -- 11.31.1 Mechanism of action -- 11.31.2 Binding mode analysis -- 11.32 Ribociclib -- 11.32.1 Mechanism of action -- 11.32.2 Binding mode analysis -- 11.33 Risperidone -- 11.33.1 Mechanism of action -- 11.33.2 Binding mode analysis -- 11.34 Ruxolitinib.
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11.34.1 Mechanism of action.
Additional Edition:
Print version: Kumar, Raj Fused Pyrimidine-Based Drug Discovery San Diego : Elsevier,c2022 ISBN 9780443186165
Language:
English
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