Kooperativer Bibliotheksverbund

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Format: 1 online resource (xxvi, 961 pages)

Edition: First edition.

ISBN: 9780443186127 , 044318612X

Content: 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 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.

Note: Front Cover -- Privileged Scaffolds in Drug Discovery -- Privileged Scaffolds in Drug Discovery -- Copyright -- Contents -- List of contributors -- Preface -- Introduction -- 1 - Thiazole, a privileged scaffold in drug discovery -- 1. Introduction -- 2. Thiazole derivatives as therapeutic agents -- 2.1 Second-generation cephalosporin antibiotics containing thiazole moiety -- 2.2 Third-generation cephalosporin antibiotics containing thiazole substituent -- 2.3 Aminothiazole-containing third-generation cephalosporins for veterinary use -- 2.4 Cephalosporin antibiotics with aminothiazole group used in prodrug forms -- 2.5 Fourth-generation cephalosporin antibiotics containing thiazole nucleus -- 2.6 Fifth-generation cephalosporin antibiotics and monobactams containing aminothiazole group -- 2.7 Thiazole-containing natural products as antimicrobial agents -- 2.8 Antifungal and antiprotozoal agents containing thiazole nucleus -- 2.9 Thiazole derivatives as antifungal and antituberculosis agents -- 2.10 Thiazole derivatives as anticancer drugs -- 2.11 Thiazole-containing antiproliferative agents -- 2.12 Thiazole-containing drugs to treat inflammatory and blood-borne diseases -- 2.13 Thiazole derivative to treat urologic and neurologic disorders -- 2.14 Miscellaneous drugs and useful compounds containing thiazole nucleus -- 2.15 Thiazole-containing essential bioactive compounds -- 3. Conclusions -- Acknowledgments -- References -- 2 - Chalcones: Diverse biological activities and structure-activity relationships -- 1. Background -- 2. Biological activities of chalcone derivatives -- 2.1 Anticancer activity -- 2.1.1 Chalcone-azole hybrids -- 2.1.2 Chalcone-furan/thiophene hybrids -- 2.1.3 Chalcone-indole hybrids -- 2.1.4 Chalcone-pyridine hybrids -- 2.2 Antiinflammatory and antioxidant activities -- 2.2.1 Simple chalcone compounds -- 2.2.2 Licochalcone B. , 2.2.3 Licochalcones A and C -- 2.3 Neurodegenerative diseases -- 2.3.1 Trihydroxylated chalcone -- 2.3.2 Imidazole-containing chalcones -- 2.3.3 Halogen-substituted chalcone -- 2.3.4 Chalcone derivatives with di-O-alkylamine substituents -- 2.3.5 Flurbiprofen-chalcone hybrids -- 2.4 Antimalarial activity -- 2.4.1 Chloroquine-containing chalcone analogs -- 2.4.2 Chloroquine-triazole-chalcone hybrids -- 2.4.3 Acetylanine-chalcone hybrids -- 2.5 Antibacterial activity -- 2.5.1 Cationic chalcone derivatives -- 2.5.2 Fluorinated chalcone-triazole hybrids -- 2.5.3 Indole-chalcones -- 2.5.4 Xanthoangelol B derivative -- 2.6 Antiviral activity -- 2.6.1 Alkyl chalcone -- 2.6.2 Licochalcone A -- 2.7 Antidiabetic activity -- 3. Conclusion -- 3.1 Financial and competing interests disclosure -- References -- 3 - Privileged chalcone scaffolds in drug discovery -- 1. Introduction -- 2. Simple chalcones classified by representative mechanisms of action -- 2.1 Michael acceptor-related targeting simple chalcones -- 2.1.1 Targeting IκB kinases -- 2.1.2 Targeting thioredoxin reductase -- 2.1.3 Targeting Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2-antioxidant response element pathway -- 2.2 Other targeting simple chalcones -- 2.2.1 Targeting microtubule formation -- 2.2.2 Targeting ATP-binding cassette G2 -- 2.2.3 Targeting RTKs (receptor tyrosine kinase) -- 2.2.4 Targeting aldose reductase -- 2.2.5 Targeting cyclooxygenase -- 3. Representative hybrid chalcones -- 3.1 Fused hybrids -- 3.1.1 Coumarin-chalcones -- 3.1.2 Indole-chalcones -- 3.1.3 Chalcone-quinoxaline hybrids -- 3.1.4 Other fused hybrid chalcones -- 3.2 Hybrids using linkages -- 3.2.1 Using an amide as a linker -- 3.2.2 Using a diol as a linker -- 3.2.3 Using an ester or ether as a linker -- 3.2.4 Using 1,2,3-triazole as a linker -- 3.2.5 Other linkers. , 4. Conclusions and perspectives -- Acknowledgments -- References -- 4 - The N-sulfonyl carboxamide moiety as a privileged structure in approved drugsa -- 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 -- Acknowledgments -- References -- 5 - Scaffolds in cytotoxic drugs and novel antitumor molecules interacting with nucleic acids -- 1. DNA intercalators -- 1.1 Ellipticine and its derivatives -- 1.2 Echinomycin and actinomycin -- 2. Topoisomerase inhibitors -- 2.1 Topoisomerase 1 poisons from natural products and their derivatives -- 2.1.1 Camptothecin and its derivatives -- 2.1.2 Nitidine, indenoisoquinoline, lamellarin, and aromathecins -- 2.1.3 Evodiamine and indolocarbazoles -- 2.1.4 Thaspine, kakuol, and pinostrobin -- 2.2 Topoisomerase 1 catalytic inhibitors from natural products and their derivatives -- 2.2.1 β-Lapachone -- 2.2.2 Berberine -- 2.2.3 Sulfoquinovosyl diacylglyceride -- 2.2.4 Globulusal A and flavonoids -- 2.3 Marine natural products as topoisomerase 1 inhibitors -- 2.4 Topoisomerase 2 inhibitors from natural products -- 2.4.1 Podophyllotoxin and its analogs -- 2.4.2 Anthracycline antibiotics and analogs -- 3. G-quadruplex ligands -- 3.1 Telomestatin -- 3.2 Cryptolepine -- 3.3 Schizocommunin -- 3.4 Isaindigotone -- 3.5 Berberine and its analogs -- 3.6 Other natural scaffolds of G4 ligands -- References -- 6 - Triazoles: a privileged scaffold in drug design and novel drug discovery -- 1. Introduction -- 2. 1,2,3-Triazole as bioisosteres -- 2.1 1,2,3-Triazole as amide group bioisosteres -- 2.2 1,2,3-Triazole as heterocycle bioisosteres -- 2.3 1,2,3-Triazole as ester group bioisosteres -- 2.4 1,2,3-Triazole as carboxyl group bioisosteres. , 2.5 1,2,3-Triazole as bioisostere for other groups -- 3. Biological significance -- 3.1 Anticancer activity -- 3.2 Antimicrobial activity -- 3.3 Other activities -- 4. Conclusions and prospects -- Acknowledgments -- References -- 7 - Oxazolidinone scaffolds in drug discovery and development -- 1. Introduction -- 2. Launched oxazolidinone antibacterial drugs -- 2.1 Linezolid -- 2.2 Tedizolid -- 3. Modification of linezolid-based oxazolidinone medications -- 3.1 Morpholine ring/C-5 position modifications -- 3.1.1 Morpholine ring modification -- 3.1.2 C-5 modification -- 3.2 Concurrent alterations to C-5 site and morpholine ring -- 3.2.1 Oxazolidinone-biphenyl chalcone hybrid derivative compounds -- 3.2.2 Derivatives of spiropyrimidinetrione oxazolidinone -- 3.2.3 [1,2,5]Triazepane or [1,2,5]oxadiazepane oxazolidinone compounds -- 3.2.4 C-Ring heteroaromatic antibacterial oxazolidinones -- 3.2.5 N-Substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinone derivatives -- 3.2.6 Replaced ligustrazine C-ring oxazolidinone antibiotics -- 3.2.7 Silicon-containing oxazolidinone antibiotics -- 3.2.8 Antibiotic oxazolidinones containing dihydropyridone C-ring unit -- 3.3 Derivatives of tricyclic fused oxazolidinones -- 3.3.1 (Pyridin-3-yl)benzo[1,4]oxazinyl-oxazolidinones -- 3.3.2 (Tetrahydropyridine-4-yl)benzo[1,4]oxazinyl-oxazolidinones -- 3.3.3 Thiomorpholine benzo[1,4]oxazinyl-oxazolidinones -- 3.3.4 Benzo[1,3]oxazinyl-oxazolidinones -- 4. Other novel oxazolidinone derivatives -- 4.1 Azetidinone moieties -- 4.2 Motifs of amide, sulfonamide, and thiourea -- 4.3 Chloroquinoline moieties -- 4.4 Thiazole hybrid moieties -- 4.5 Oxazolidinone derivative-based UDP-3-O-acyl-N-acetylglucosamine deacetylase inhibitor -- 4.6 3-Amino-2-oxazolidinone derivatives -- 5. Effects of oxazolidinone derivatives on other diseases -- 6. Summary and perspective -- References. , 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 -- 3.1 Antitumor agents -- 3.1.1 Natural derivatives -- 3.1.2 Kinase inhibitors -- 3.1.3 Histone deacetylase inhibitors -- 3.1.4 Multitargeting agents -- 3.2 Antimicrobial agents -- 3.2.1 Natural antimicrobial agents -- 3.2.2 Synthetic antimicrobial agents -- 3.3 Antiviral agents -- 3.3.1 Anti-human immunodeficiency virus agents -- 3.3.2 Anti-herpes simplex virus agents -- 3.3.3 Anti-hepatitis C virus agents -- 3.3.4 Other antiviral agents -- 3.4 Antiinflammatory agents -- 3.5 Drugs for neurologic disease -- 3.6 Drugs for chronic disease -- 3.7 Other therapeutic applications -- 4. Conclusion and future perspectives -- References -- 9 - Cyanopyridine as a privileged scaffold in drug discovery -- 1. Introduction -- 2. Synthesis of cyanopyridine derivatives -- 2.1 Application of cyanopyridines in anticancer drugs -- 2.1.1 SRC/ABL dual inhibitor -- 2.2 Epidermal growth factor receptor inhibitor -- 2.3 Epidermal growth factor receptor/human epidermal growth factor receptor-2 dual inhibitor -- 2.4 Checkpoint kinase 1 inhibitor -- 2.5 FER inhibitor -- 2.6 PIM-1 inhibitor -- 2.7 Farnesyltransferase inhibitor -- 2.8 B-cell lymphoma 6 inhibitor -- 2.9 Androgen receptor antagonist -- 2.10 DNA methyltransferase 1 inhibitor -- 2.11 Survivin dimerization modulator -- 2.12 Isocitrate dehydrogenase 1 inhibitor -- 2.13 Rearranged during transfection (RET) inhibitor -- 2.14 JAK2 inhibitor -- 2.15 CDK2 inhibitor -- 2.16 General control nonrepressed protein 5 inhibitor -- 2.17 Application of cyanopyridines in antiinflammatory areas -- 2.17.1 IκB kinase β inhibitor -- 2.18 Mitogen-activated protein kinase-activated protein kinase 2 inhibitor -- 2.19 Cyclooxygenase-2 inhibitor. , 2.20 Phosphodiesterase-4 inhibitor.

Additional Edition: Print version: Yu, Bin Privileged Scaffolds in Drug Discovery San Diego : Elsevier Science & Technology,c2023 ISBN 9780443186110

Language: English

UID:

ISBN: 0-443-18612-X , 9780443186127 , 044318612X

Content: 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 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.

Note: Front Cover -- Privileged Scaffolds in Drug Discovery -- Privileged Scaffolds in Drug Discovery -- Copyright -- Contents -- List of contributors -- Preface -- Introduction -- 1 - Thiazole, a privileged scaffold in drug discovery -- 1. Introduction -- 2. Thiazole derivatives as therapeutic agents -- 2.1 Second-generation cephalosporin antibiotics containing thiazole moiety -- 2.2 Third-generation cephalosporin antibiotics containing thiazole substituent -- 2.3 Aminothiazole-containing third-generation cephalosporins for veterinary use -- 2.4 Cephalosporin antibiotics with aminothiazole group used in prodrug forms -- 2.5 Fourth-generation cephalosporin antibiotics containing thiazole nucleus -- 2.6 Fifth-generation cephalosporin antibiotics and monobactams containing aminothiazole group -- 2.7 Thiazole-containing natural products as antimicrobial agents -- 2.8 Antifungal and antiprotozoal agents containing thiazole nucleus -- 2.9 Thiazole derivatives as antifungal and antituberculosis agents -- 2.10 Thiazole derivatives as anticancer drugs -- 2.11 Thiazole-containing antiproliferative agents -- 2.12 Thiazole-containing drugs to treat inflammatory and blood-borne diseases -- 2.13 Thiazole derivative to treat urologic and neurologic disorders -- 2.14 Miscellaneous drugs and useful compounds containing thiazole nucleus -- 2.15 Thiazole-containing essential bioactive compounds -- 3. Conclusions -- Acknowledgments -- References -- 2 - Chalcones: Diverse biological activities and structure-activity relationships -- 1. Background -- 2. Biological activities of chalcone derivatives -- 2.1 Anticancer activity -- 2.1.1 Chalcone-azole hybrids -- 2.1.2 Chalcone-furan/thiophene hybrids -- 2.1.3 Chalcone-indole hybrids -- 2.1.4 Chalcone-pyridine hybrids -- 2.2 Antiinflammatory and antioxidant activities -- 2.2.1 Simple chalcone compounds -- 2.2.2 Licochalcone B. , 2.2.3 Licochalcones A and C -- 2.3 Neurodegenerative diseases -- 2.3.1 Trihydroxylated chalcone -- 2.3.2 Imidazole-containing chalcones -- 2.3.3 Halogen-substituted chalcone -- 2.3.4 Chalcone derivatives with di-O-alkylamine substituents -- 2.3.5 Flurbiprofen-chalcone hybrids -- 2.4 Antimalarial activity -- 2.4.1 Chloroquine-containing chalcone analogs -- 2.4.2 Chloroquine-triazole-chalcone hybrids -- 2.4.3 Acetylanine-chalcone hybrids -- 2.5 Antibacterial activity -- 2.5.1 Cationic chalcone derivatives -- 2.5.2 Fluorinated chalcone-triazole hybrids -- 2.5.3 Indole-chalcones -- 2.5.4 Xanthoangelol B derivative -- 2.6 Antiviral activity -- 2.6.1 Alkyl chalcone -- 2.6.2 Licochalcone A -- 2.7 Antidiabetic activity -- 3. Conclusion -- 3.1 Financial and competing interests disclosure -- References -- 3 - Privileged chalcone scaffolds in drug discovery -- 1. Introduction -- 2. Simple chalcones classified by representative mechanisms of action -- 2.1 Michael acceptor-related targeting simple chalcones -- 2.1.1 Targeting IκB kinases -- 2.1.2 Targeting thioredoxin reductase -- 2.1.3 Targeting Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2-antioxidant response element pathway -- 2.2 Other targeting simple chalcones -- 2.2.1 Targeting microtubule formation -- 2.2.2 Targeting ATP-binding cassette G2 -- 2.2.3 Targeting RTKs (receptor tyrosine kinase) -- 2.2.4 Targeting aldose reductase -- 2.2.5 Targeting cyclooxygenase -- 3. Representative hybrid chalcones -- 3.1 Fused hybrids -- 3.1.1 Coumarin-chalcones -- 3.1.2 Indole-chalcones -- 3.1.3 Chalcone-quinoxaline hybrids -- 3.1.4 Other fused hybrid chalcones -- 3.2 Hybrids using linkages -- 3.2.1 Using an amide as a linker -- 3.2.2 Using a diol as a linker -- 3.2.3 Using an ester or ether as a linker -- 3.2.4 Using 1,2,3-triazole as a linker -- 3.2.5 Other linkers. , 4. Conclusions and perspectives -- Acknowledgments -- References -- 4 - The N-sulfonyl carboxamide moiety as a privileged structure in approved drugsa -- 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 -- Acknowledgments -- References -- 5 - Scaffolds in cytotoxic drugs and novel antitumor molecules interacting with nucleic acids -- 1. DNA intercalators -- 1.1 Ellipticine and its derivatives -- 1.2 Echinomycin and actinomycin -- 2. Topoisomerase inhibitors -- 2.1 Topoisomerase 1 poisons from natural products and their derivatives -- 2.1.1 Camptothecin and its derivatives -- 2.1.2 Nitidine, indenoisoquinoline, lamellarin, and aromathecins -- 2.1.3 Evodiamine and indolocarbazoles -- 2.1.4 Thaspine, kakuol, and pinostrobin -- 2.2 Topoisomerase 1 catalytic inhibitors from natural products and their derivatives -- 2.2.1 β-Lapachone -- 2.2.2 Berberine -- 2.2.3 Sulfoquinovosyl diacylglyceride -- 2.2.4 Globulusal A and flavonoids -- 2.3 Marine natural products as topoisomerase 1 inhibitors -- 2.4 Topoisomerase 2 inhibitors from natural products -- 2.4.1 Podophyllotoxin and its analogs -- 2.4.2 Anthracycline antibiotics and analogs -- 3. G-quadruplex ligands -- 3.1 Telomestatin -- 3.2 Cryptolepine -- 3.3 Schizocommunin -- 3.4 Isaindigotone -- 3.5 Berberine and its analogs -- 3.6 Other natural scaffolds of G4 ligands -- References -- 6 - Triazoles: a privileged scaffold in drug design and novel drug discovery -- 1. Introduction -- 2. 1,2,3-Triazole as bioisosteres -- 2.1 1,2,3-Triazole as amide group bioisosteres -- 2.2 1,2,3-Triazole as heterocycle bioisosteres -- 2.3 1,2,3-Triazole as ester group bioisosteres -- 2.4 1,2,3-Triazole as carboxyl group bioisosteres. , 2.5 1,2,3-Triazole as bioisostere for other groups -- 3. Biological significance -- 3.1 Anticancer activity -- 3.2 Antimicrobial activity -- 3.3 Other activities -- 4. Conclusions and prospects -- Acknowledgments -- References -- 7 - Oxazolidinone scaffolds in drug discovery and development -- 1. Introduction -- 2. Launched oxazolidinone antibacterial drugs -- 2.1 Linezolid -- 2.2 Tedizolid -- 3. Modification of linezolid-based oxazolidinone medications -- 3.1 Morpholine ring/C-5 position modifications -- 3.1.1 Morpholine ring modification -- 3.1.2 C-5 modification -- 3.2 Concurrent alterations to C-5 site and morpholine ring -- 3.2.1 Oxazolidinone-biphenyl chalcone hybrid derivative compounds -- 3.2.2 Derivatives of spiropyrimidinetrione oxazolidinone -- 3.2.3 [1,2,5]Triazepane or [1,2,5]oxadiazepane oxazolidinone compounds -- 3.2.4 C-Ring heteroaromatic antibacterial oxazolidinones -- 3.2.5 N-Substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinone derivatives -- 3.2.6 Replaced ligustrazine C-ring oxazolidinone antibiotics -- 3.2.7 Silicon-containing oxazolidinone antibiotics -- 3.2.8 Antibiotic oxazolidinones containing dihydropyridone C-ring unit -- 3.3 Derivatives of tricyclic fused oxazolidinones -- 3.3.1 (Pyridin-3-yl)benzo[1,4]oxazinyl-oxazolidinones -- 3.3.2 (Tetrahydropyridine-4-yl)benzo[1,4]oxazinyl-oxazolidinones -- 3.3.3 Thiomorpholine benzo[1,4]oxazinyl-oxazolidinones -- 3.3.4 Benzo[1,3]oxazinyl-oxazolidinones -- 4. Other novel oxazolidinone derivatives -- 4.1 Azetidinone moieties -- 4.2 Motifs of amide, sulfonamide, and thiourea -- 4.3 Chloroquinoline moieties -- 4.4 Thiazole hybrid moieties -- 4.5 Oxazolidinone derivative-based UDP-3-O-acyl-N-acetylglucosamine deacetylase inhibitor -- 4.6 3-Amino-2-oxazolidinone derivatives -- 5. Effects of oxazolidinone derivatives on other diseases -- 6. Summary and perspective -- References. , 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 -- 3.1 Antitumor agents -- 3.1.1 Natural derivatives -- 3.1.2 Kinase inhibitors -- 3.1.3 Histone deacetylase inhibitors -- 3.1.4 Multitargeting agents -- 3.2 Antimicrobial agents -- 3.2.1 Natural antimicrobial agents -- 3.2.2 Synthetic antimicrobial agents -- 3.3 Antiviral agents -- 3.3.1 Anti-human immunodeficiency virus agents -- 3.3.2 Anti-herpes simplex virus agents -- 3.3.3 Anti-hepatitis C virus agents -- 3.3.4 Other antiviral agents -- 3.4 Antiinflammatory agents -- 3.5 Drugs for neurologic disease -- 3.6 Drugs for chronic disease -- 3.7 Other therapeutic applications -- 4. Conclusion and future perspectives -- References -- 9 - Cyanopyridine as a privileged scaffold in drug discovery -- 1. Introduction -- 2. Synthesis of cyanopyridine derivatives -- 2.1 Application of cyanopyridines in anticancer drugs -- 2.1.1 SRC/ABL dual inhibitor -- 2.2 Epidermal growth factor receptor inhibitor -- 2.3 Epidermal growth factor receptor/human epidermal growth factor receptor-2 dual inhibitor -- 2.4 Checkpoint kinase 1 inhibitor -- 2.5 FER inhibitor -- 2.6 PIM-1 inhibitor -- 2.7 Farnesyltransferase inhibitor -- 2.8 B-cell lymphoma 6 inhibitor -- 2.9 Androgen receptor antagonist -- 2.10 DNA methyltransferase 1 inhibitor -- 2.11 Survivin dimerization modulator -- 2.12 Isocitrate dehydrogenase 1 inhibitor -- 2.13 Rearranged during transfection (RET) inhibitor -- 2.14 JAK2 inhibitor -- 2.15 CDK2 inhibitor -- 2.16 General control nonrepressed protein 5 inhibitor -- 2.17 Application of cyanopyridines in antiinflammatory areas -- 2.17.1 IκB kinase β inhibitor -- 2.18 Mitogen-activated protein kinase-activated protein kinase 2 inhibitor -- 2.19 Cyclooxygenase-2 inhibitor. , 2.20 Phosphodiesterase-4 inhibitor.

Additional Edition: Print version: Yu, Bin Privileged Scaffolds in Drug Discovery San Diego : Elsevier Science & Technology,c2023 ISBN 9780443186110

Language: English

UID:

ISBN: 0-443-18612-X , 9780443186127 , 044318612X

Content: 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 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.

Note: Front Cover -- Privileged Scaffolds in Drug Discovery -- Privileged Scaffolds in Drug Discovery -- Copyright -- Contents -- List of contributors -- Preface -- Introduction -- 1 - Thiazole, a privileged scaffold in drug discovery -- 1. Introduction -- 2. Thiazole derivatives as therapeutic agents -- 2.1 Second-generation cephalosporin antibiotics containing thiazole moiety -- 2.2 Third-generation cephalosporin antibiotics containing thiazole substituent -- 2.3 Aminothiazole-containing third-generation cephalosporins for veterinary use -- 2.4 Cephalosporin antibiotics with aminothiazole group used in prodrug forms -- 2.5 Fourth-generation cephalosporin antibiotics containing thiazole nucleus -- 2.6 Fifth-generation cephalosporin antibiotics and monobactams containing aminothiazole group -- 2.7 Thiazole-containing natural products as antimicrobial agents -- 2.8 Antifungal and antiprotozoal agents containing thiazole nucleus -- 2.9 Thiazole derivatives as antifungal and antituberculosis agents -- 2.10 Thiazole derivatives as anticancer drugs -- 2.11 Thiazole-containing antiproliferative agents -- 2.12 Thiazole-containing drugs to treat inflammatory and blood-borne diseases -- 2.13 Thiazole derivative to treat urologic and neurologic disorders -- 2.14 Miscellaneous drugs and useful compounds containing thiazole nucleus -- 2.15 Thiazole-containing essential bioactive compounds -- 3. Conclusions -- Acknowledgments -- References -- 2 - Chalcones: Diverse biological activities and structure-activity relationships -- 1. Background -- 2. Biological activities of chalcone derivatives -- 2.1 Anticancer activity -- 2.1.1 Chalcone-azole hybrids -- 2.1.2 Chalcone-furan/thiophene hybrids -- 2.1.3 Chalcone-indole hybrids -- 2.1.4 Chalcone-pyridine hybrids -- 2.2 Antiinflammatory and antioxidant activities -- 2.2.1 Simple chalcone compounds -- 2.2.2 Licochalcone B. , 2.2.3 Licochalcones A and C -- 2.3 Neurodegenerative diseases -- 2.3.1 Trihydroxylated chalcone -- 2.3.2 Imidazole-containing chalcones -- 2.3.3 Halogen-substituted chalcone -- 2.3.4 Chalcone derivatives with di-O-alkylamine substituents -- 2.3.5 Flurbiprofen-chalcone hybrids -- 2.4 Antimalarial activity -- 2.4.1 Chloroquine-containing chalcone analogs -- 2.4.2 Chloroquine-triazole-chalcone hybrids -- 2.4.3 Acetylanine-chalcone hybrids -- 2.5 Antibacterial activity -- 2.5.1 Cationic chalcone derivatives -- 2.5.2 Fluorinated chalcone-triazole hybrids -- 2.5.3 Indole-chalcones -- 2.5.4 Xanthoangelol B derivative -- 2.6 Antiviral activity -- 2.6.1 Alkyl chalcone -- 2.6.2 Licochalcone A -- 2.7 Antidiabetic activity -- 3. Conclusion -- 3.1 Financial and competing interests disclosure -- References -- 3 - Privileged chalcone scaffolds in drug discovery -- 1. Introduction -- 2. Simple chalcones classified by representative mechanisms of action -- 2.1 Michael acceptor-related targeting simple chalcones -- 2.1.1 Targeting IκB kinases -- 2.1.2 Targeting thioredoxin reductase -- 2.1.3 Targeting Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2-antioxidant response element pathway -- 2.2 Other targeting simple chalcones -- 2.2.1 Targeting microtubule formation -- 2.2.2 Targeting ATP-binding cassette G2 -- 2.2.3 Targeting RTKs (receptor tyrosine kinase) -- 2.2.4 Targeting aldose reductase -- 2.2.5 Targeting cyclooxygenase -- 3. Representative hybrid chalcones -- 3.1 Fused hybrids -- 3.1.1 Coumarin-chalcones -- 3.1.2 Indole-chalcones -- 3.1.3 Chalcone-quinoxaline hybrids -- 3.1.4 Other fused hybrid chalcones -- 3.2 Hybrids using linkages -- 3.2.1 Using an amide as a linker -- 3.2.2 Using a diol as a linker -- 3.2.3 Using an ester or ether as a linker -- 3.2.4 Using 1,2,3-triazole as a linker -- 3.2.5 Other linkers. , 4. Conclusions and perspectives -- Acknowledgments -- References -- 4 - The N-sulfonyl carboxamide moiety as a privileged structure in approved drugsa -- 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 -- Acknowledgments -- References -- 5 - Scaffolds in cytotoxic drugs and novel antitumor molecules interacting with nucleic acids -- 1. DNA intercalators -- 1.1 Ellipticine and its derivatives -- 1.2 Echinomycin and actinomycin -- 2. Topoisomerase inhibitors -- 2.1 Topoisomerase 1 poisons from natural products and their derivatives -- 2.1.1 Camptothecin and its derivatives -- 2.1.2 Nitidine, indenoisoquinoline, lamellarin, and aromathecins -- 2.1.3 Evodiamine and indolocarbazoles -- 2.1.4 Thaspine, kakuol, and pinostrobin -- 2.2 Topoisomerase 1 catalytic inhibitors from natural products and their derivatives -- 2.2.1 β-Lapachone -- 2.2.2 Berberine -- 2.2.3 Sulfoquinovosyl diacylglyceride -- 2.2.4 Globulusal A and flavonoids -- 2.3 Marine natural products as topoisomerase 1 inhibitors -- 2.4 Topoisomerase 2 inhibitors from natural products -- 2.4.1 Podophyllotoxin and its analogs -- 2.4.2 Anthracycline antibiotics and analogs -- 3. G-quadruplex ligands -- 3.1 Telomestatin -- 3.2 Cryptolepine -- 3.3 Schizocommunin -- 3.4 Isaindigotone -- 3.5 Berberine and its analogs -- 3.6 Other natural scaffolds of G4 ligands -- References -- 6 - Triazoles: a privileged scaffold in drug design and novel drug discovery -- 1. Introduction -- 2. 1,2,3-Triazole as bioisosteres -- 2.1 1,2,3-Triazole as amide group bioisosteres -- 2.2 1,2,3-Triazole as heterocycle bioisosteres -- 2.3 1,2,3-Triazole as ester group bioisosteres -- 2.4 1,2,3-Triazole as carboxyl group bioisosteres. , 2.5 1,2,3-Triazole as bioisostere for other groups -- 3. Biological significance -- 3.1 Anticancer activity -- 3.2 Antimicrobial activity -- 3.3 Other activities -- 4. Conclusions and prospects -- Acknowledgments -- References -- 7 - Oxazolidinone scaffolds in drug discovery and development -- 1. Introduction -- 2. Launched oxazolidinone antibacterial drugs -- 2.1 Linezolid -- 2.2 Tedizolid -- 3. Modification of linezolid-based oxazolidinone medications -- 3.1 Morpholine ring/C-5 position modifications -- 3.1.1 Morpholine ring modification -- 3.1.2 C-5 modification -- 3.2 Concurrent alterations to C-5 site and morpholine ring -- 3.2.1 Oxazolidinone-biphenyl chalcone hybrid derivative compounds -- 3.2.2 Derivatives of spiropyrimidinetrione oxazolidinone -- 3.2.3 [1,2,5]Triazepane or [1,2,5]oxadiazepane oxazolidinone compounds -- 3.2.4 C-Ring heteroaromatic antibacterial oxazolidinones -- 3.2.5 N-Substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinone derivatives -- 3.2.6 Replaced ligustrazine C-ring oxazolidinone antibiotics -- 3.2.7 Silicon-containing oxazolidinone antibiotics -- 3.2.8 Antibiotic oxazolidinones containing dihydropyridone C-ring unit -- 3.3 Derivatives of tricyclic fused oxazolidinones -- 3.3.1 (Pyridin-3-yl)benzo[1,4]oxazinyl-oxazolidinones -- 3.3.2 (Tetrahydropyridine-4-yl)benzo[1,4]oxazinyl-oxazolidinones -- 3.3.3 Thiomorpholine benzo[1,4]oxazinyl-oxazolidinones -- 3.3.4 Benzo[1,3]oxazinyl-oxazolidinones -- 4. Other novel oxazolidinone derivatives -- 4.1 Azetidinone moieties -- 4.2 Motifs of amide, sulfonamide, and thiourea -- 4.3 Chloroquinoline moieties -- 4.4 Thiazole hybrid moieties -- 4.5 Oxazolidinone derivative-based UDP-3-O-acyl-N-acetylglucosamine deacetylase inhibitor -- 4.6 3-Amino-2-oxazolidinone derivatives -- 5. Effects of oxazolidinone derivatives on other diseases -- 6. Summary and perspective -- References. , 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 -- 3.1 Antitumor agents -- 3.1.1 Natural derivatives -- 3.1.2 Kinase inhibitors -- 3.1.3 Histone deacetylase inhibitors -- 3.1.4 Multitargeting agents -- 3.2 Antimicrobial agents -- 3.2.1 Natural antimicrobial agents -- 3.2.2 Synthetic antimicrobial agents -- 3.3 Antiviral agents -- 3.3.1 Anti-human immunodeficiency virus agents -- 3.3.2 Anti-herpes simplex virus agents -- 3.3.3 Anti-hepatitis C virus agents -- 3.3.4 Other antiviral agents -- 3.4 Antiinflammatory agents -- 3.5 Drugs for neurologic disease -- 3.6 Drugs for chronic disease -- 3.7 Other therapeutic applications -- 4. Conclusion and future perspectives -- References -- 9 - Cyanopyridine as a privileged scaffold in drug discovery -- 1. Introduction -- 2. Synthesis of cyanopyridine derivatives -- 2.1 Application of cyanopyridines in anticancer drugs -- 2.1.1 SRC/ABL dual inhibitor -- 2.2 Epidermal growth factor receptor inhibitor -- 2.3 Epidermal growth factor receptor/human epidermal growth factor receptor-2 dual inhibitor -- 2.4 Checkpoint kinase 1 inhibitor -- 2.5 FER inhibitor -- 2.6 PIM-1 inhibitor -- 2.7 Farnesyltransferase inhibitor -- 2.8 B-cell lymphoma 6 inhibitor -- 2.9 Androgen receptor antagonist -- 2.10 DNA methyltransferase 1 inhibitor -- 2.11 Survivin dimerization modulator -- 2.12 Isocitrate dehydrogenase 1 inhibitor -- 2.13 Rearranged during transfection (RET) inhibitor -- 2.14 JAK2 inhibitor -- 2.15 CDK2 inhibitor -- 2.16 General control nonrepressed protein 5 inhibitor -- 2.17 Application of cyanopyridines in antiinflammatory areas -- 2.17.1 IκB kinase β inhibitor -- 2.18 Mitogen-activated protein kinase-activated protein kinase 2 inhibitor -- 2.19 Cyclooxygenase-2 inhibitor. , 2.20 Phosphodiesterase-4 inhibitor.

Additional Edition: Print version: Yu, Bin Privileged Scaffolds in Drug Discovery San Diego : Elsevier Science & Technology,c2023 ISBN 9780443186110

Language: English