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  1. Article ; Online: Novel 2-indolinone derivatives as promising agents against respiratory syncytial and yellow fever viruses.

    Apaydın, Çağla Begüm / Göktaş, Füsun / Naesens, Lieve / Karalı, Nilgün

    Future medicinal chemistry

    2024  Volume 16, Issue 4, Page(s) 295–310

    Abstract: Background: ...

    Abstract Background:
    MeSH term(s) Humans ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; Halogens ; Sulfonamides/pharmacology ; Yellow Fever/drug therapy ; Yellow fever virus ; Indoles/chemistry ; Indoles/pharmacology
    Chemical Substances Antiviral Agents ; Halogens ; Sulfonamides ; Indoles
    Language English
    Publishing date 2024-01-30
    Publishing country England
    Document type Journal Article
    ISSN 1756-8927
    ISSN (online) 1756-8927
    DOI 10.4155/fmc-2023-0179
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Small-molecule Antiviral Agents in Ongoing Clinical Trials for COVID-19.

    Apaydın, Çağla Begüm / Çınar, Gözde / Cihan-Üstündağ, Gökçe

    Current drug targets

    2021  Volume 22, Issue 17, Page(s) 1986–2005

    Abstract: The coronavirus disease 2019 (COVID-19) pandemic, due to the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), emerged in December 2019 and has rapidly spread globally. As the confirmed number of cases has reached 83 million worldwide, ... ...

    Abstract The coronavirus disease 2019 (COVID-19) pandemic, due to the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), emerged in December 2019 and has rapidly spread globally. As the confirmed number of cases has reached 83 million worldwide, the potential severity and the deadly complications of the disease requires urgent development of effective drugs for prevention and treatment. No proven effective treatment for this virus currently exists. Most of the antiviral discovery efforts are focused on the repurposing of approved or clinical stage drugs. This review highlights the small-molecule repurposed antiviral agents that are currently under investigation in clinical trials for COVID-19. These include viral polymerase and protease inhibitors remdesivir, galidesivir, favipiravir, ribavirin, sofosbuvir, tenofovir/emtricitabine, baloxavir marboxil, EIDD-2801, lopinavir/ritonavir; virus-/host-directed viral entry and fusion inhibitors arbidol chloroquine/hydroxychloroquine, chlorpromazine, camostat mesylate, nafamostat mesylate, bromhexine and agents with diverse/unclear mechanism of actions as oseltamivir, triazavirin, ivermectin, nitazoxanide, niclosamide and BLD-2660. The published preclinical and clinical data to date on these drugs as well as the mechanisms of action are reviewed.
    MeSH term(s) Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; COVID-19/drug therapy ; Clinical Trials as Topic ; Drug Repositioning ; Humans ; Pandemics ; SARS-CoV-2/drug effects
    Chemical Substances Antiviral Agents
    Language English
    Publishing date 2021-02-15
    Publishing country United Arab Emirates
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 2064859-5
    ISSN 1873-5592 ; 1389-4501
    ISSN (online) 1873-5592
    ISSN 1389-4501
    DOI 10.2174/1389450122666210215112150
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5578: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: Synthesis, molecular modeling and cholinesterase inhibitory effects of 2-indolinone-based hydrazinecarbothioamides.

    Demir-Yazıcı, Kübra / Apaydın, Çağla Begüm / Soylu-Eter, Özge / Özsoy, Nurten / Karalı, Nilgün

    Future medicinal chemistry

    2021  Volume 13, Issue 24, Page(s) 2133–2151

    Abstract: Background: ...

    Abstract Background:
    MeSH term(s) Acetylcholinesterase/metabolism ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Butyrylcholinesterase/metabolism ; Cholinesterase Inhibitors/chemical synthesis ; Cholinesterase Inhibitors/chemistry ; Cholinesterase Inhibitors/pharmacology ; Humans ; Hydrazines/chemical synthesis ; Hydrazines/chemistry ; Hydrazines/pharmacology ; Models, Molecular ; Molecular Structure ; Oxindoles/chemistry ; Oxindoles/pharmacology ; Thioamides/chemical synthesis ; Thioamides/chemistry ; Thioamides/pharmacology
    Chemical Substances Cholinesterase Inhibitors ; Hydrazines ; Oxindoles ; Thioamides ; hydrazinecarbothioamide ; 2-oxindole (0S9338U62H) ; Acetylcholinesterase (EC 3.1.1.7) ; Butyrylcholinesterase (EC 3.1.1.8)
    Language English
    Publishing date 2021-11-10
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 1756-8927
    ISSN (online) 1756-8927
    DOI 10.4155/fmc-2021-0018
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Design, synthesis and anti-influenza virus activity of furan-substituted spirothiazolidinones.

    Apaydın, Çağla Begüm / Tansuyu, Merve / Cesur, Zafer / Naesens, Lieve / Göktaş, Füsun

    Bioorganic chemistry

    2021  Volume 112, Page(s) 104958

    Abstract: A new series of N-(3-oxo-1-thia-4-azaspiro[4.5]decan-4-yl)carboxamides have been designed, synthesized and evaluated as antiviral agents. The compounds were prepared by condensation of 2-methylfuran-3-carbohydrazide, appropriate carbonyl compounds and ... ...

    Abstract A new series of N-(3-oxo-1-thia-4-azaspiro[4.5]decan-4-yl)carboxamides have been designed, synthesized and evaluated as antiviral agents. The compounds were prepared by condensation of 2-methylfuran-3-carbohydrazide, appropriate carbonyl compounds and sulfanyl acids. The new molecules were characterized by IR,
    MeSH term(s) Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Dose-Response Relationship, Drug ; Drug Design ; Furans/chemistry ; Furans/pharmacology ; Microbial Sensitivity Tests ; Molecular Docking Simulation ; Molecular Structure ; Orthomyxoviridae/drug effects ; Spiro Compounds/chemical synthesis ; Spiro Compounds/chemistry ; Spiro Compounds/pharmacology ; Structure-Activity Relationship ; Thiazolidinediones/chemical synthesis ; Thiazolidinediones/chemistry ; Thiazolidinediones/pharmacology
    Chemical Substances Antiviral Agents ; Furans ; Spiro Compounds ; Thiazolidinediones
    Language English
    Publishing date 2021-04-30
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2021.104958
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4207: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  5. Article ; Online: Synthesis and anti-coronavirus activity of a series of 1-thia-4-azaspiro[4.5]decan-3-one derivatives.

    Apaydın, Çağla Begüm / Cesur, Nesrin / Stevaert, Annelies / Naesens, Lieve / Cesur, Zafer

    Archiv der Pharmazie

    2019  Volume 352, Issue 6, Page(s) e1800330

    Abstract: A series of 1-thia-4-azaspiro[4.5]decan-3-ones bearing an amide group at C-4 and various substitutions at C-2 and C-8 were synthesized and evaluated against human coronavirus and influenza virus. Compounds 7m, 7n, 8k, 8l, 8m, 8n, and 8p were found to ... ...

    Abstract A series of 1-thia-4-azaspiro[4.5]decan-3-ones bearing an amide group at C-4 and various substitutions at C-2 and C-8 were synthesized and evaluated against human coronavirus and influenza virus. Compounds 7m, 7n, 8k, 8l, 8m, 8n, and 8p were found to inhibit human coronavirus 229E replication. The most active compound was N-(2-methyl-8-tert-butyl-3-oxo-1-thia-4-azaspiro[4.5]decan-4-yl)-3-phenylpropanamide (8n), with an EC
    MeSH term(s) Animals ; Antiviral Agents/chemical synthesis ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; Aza Compounds/chemical synthesis ; Aza Compounds/chemistry ; Aza Compounds/pharmacology ; Coronavirus/drug effects ; Cytopathogenic Effect, Viral/drug effects ; Dogs ; Drug Design ; Fibroblasts/drug effects ; Fibroblasts/virology ; Humans ; Madin Darby Canine Kidney Cells ; Molecular Structure ; Spiro Compounds/chemical synthesis ; Spiro Compounds/chemistry ; Spiro Compounds/pharmacology ; Structure-Activity Relationship ; Virus Replication/drug effects
    Chemical Substances Antiviral Agents ; Aza Compounds ; Spiro Compounds
    Keywords covid19
    Language English
    Publishing date 2019-05-09
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 6381-2
    ISSN 1521-4184 ; 0365-6233 ; 1437-1014
    ISSN (online) 1521-4184
    ISSN 0365-6233 ; 1437-1014
    DOI 10.1002/ardp.201800330
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Uf I Zs.4: Show issues Location:
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    ab Jg. 2022: Lesesaal (EG)

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