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  1. Artikel ; Online: Antiviral Drug Discovery for the Treatment of COVID-19 Infections.

    Ng, Teresa I / Correia, Ivan / Seagal, Jane / DeGoey, David A / Schrimpf, Michael R / Hardee, David J / Noey, Elizabeth L / Kati, Warren M

    Viruses

    2022  Band 14, Heft 5

    Abstract: The coronavirus disease 2019 (COVID-19) pandemic is caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a recently emerged human coronavirus. COVID-19 vaccines have proven to be successful in protecting the vaccinated from ... ...

    Abstract The coronavirus disease 2019 (COVID-19) pandemic is caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a recently emerged human coronavirus. COVID-19 vaccines have proven to be successful in protecting the vaccinated from infection, reducing the severity of disease, and deterring the transmission of infection. However, COVID-19 vaccination faces many challenges, such as the decline in vaccine-induced immunity over time, and the decrease in potency against some SARS-CoV-2 variants including the recently emerged Omicron variant, resulting in breakthrough infections. The challenges that COVID-19 vaccination is facing highlight the importance of the discovery of antivirals to serve as another means to tackle the pandemic. To date, neutralizing antibodies that block viral entry by targeting the viral spike protein make up the largest class of antivirals that has received US FDA emergency use authorization (EUA) for COVID-19 treatment. In addition to the spike protein, other key targets for the discovery of direct-acting antivirals include viral enzymes that are essential for SARS-CoV-2 replication, such as RNA-dependent RNA polymerase and proteases, as judged by US FDA approval for remdesivir, and EUA for Paxlovid (nirmatrelvir + ritonavir) for treating COVID-19 infections. This review presents an overview of the current status and future direction of antiviral drug discovery for treating SARS-CoV-2 infections, covering important antiviral targets such as the viral spike protein, non-structural protein (nsp) 3 papain-like protease, nsp5 main protease, and the nsp12/nsp7/nsp8 RNA-dependent RNA polymerase complex.
    Mesh-Begriff(e) Antiviral Agents/pharmacology ; COVID-19/drug therapy ; COVID-19 Vaccines ; Coronavirus 3C Proteases/antagonists & inhibitors ; Drug Discovery ; Humans ; RNA-Dependent RNA Polymerase/antagonists & inhibitors ; SARS-CoV-2 ; Spike Glycoprotein, Coronavirus/antagonists & inhibitors ; Viral Proteins/metabolism
    Chemische Substanzen Antiviral Agents ; COVID-19 Vaccines ; Spike Glycoprotein, Coronavirus ; Viral Proteins ; spike protein, SARS-CoV-2 ; RNA-Dependent RNA Polymerase (EC 2.7.7.48) ; 3C-like proteinase, SARS-CoV-2 (EC 3.4.22.-) ; Coronavirus 3C Proteases (EC 3.4.22.28)
    Sprache Englisch
    Erscheinungsdatum 2022-05-04
    Erscheinungsland Switzerland
    Dokumenttyp Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ZDB-ID 2516098-9
    ISSN 1999-4915 ; 1999-4915
    ISSN (online) 1999-4915
    ISSN 1999-4915
    DOI 10.3390/v14050961
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  2. Artikel: Asymmetric synthesis of pharmaceutically relevant 1-aryl-2-heteroaryl- and 1,2-diheteroarylcyclopropane-1-carboxylates.

    Sharland, Jack C / Wei, Bo / Hardee, David J / Hodges, Timothy R / Gong, Wei / Voight, Eric A / Davies, Huw M L

    Chemical science

    2021  Band 12, Heft 33, Seite(n) 11181–11190

    Abstract: This study describes general methods for the enantioselective syntheses of pharmaceutically relevant 1-aryl-2-heteroaryl- and 1,2-diheteroarylcyclopropane-1-carboxylates through dirhodium tetracarboxylate-catalysed asymmetric cyclopropanation of vinyl ... ...

    Abstract This study describes general methods for the enantioselective syntheses of pharmaceutically relevant 1-aryl-2-heteroaryl- and 1,2-diheteroarylcyclopropane-1-carboxylates through dirhodium tetracarboxylate-catalysed asymmetric cyclopropanation of vinyl heterocycles with aryl- or heteroaryldiazoacetates. The reactions are highly diastereoselective and high asymmetric induction could be achieved using either (
    Sprache Englisch
    Erscheinungsdatum 2021-07-27
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 2559110-1
    ISSN 2041-6539 ; 2041-6520
    ISSN (online) 2041-6539
    ISSN 2041-6520
    DOI 10.1039/d1sc02474d
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  3. Artikel ; Online: Lanthanum(III) triflate-catalyzed cyclopropanation via intramolecular methylene transfer.

    Hardee, David J / Lambert, Tristan H

    Journal of the American Chemical Society

    2009  Band 131, Heft 22, Seite(n) 7536–7537

    Abstract: A new method for cyclopropanation involving intramolecular methylene transfer from an epoxide to an olefin has been developed. This La(OTf)(3)-catalyzed process proceeds with good efficiency and with high stereoselectivity. A range of examples ... ...

    Abstract A new method for cyclopropanation involving intramolecular methylene transfer from an epoxide to an olefin has been developed. This La(OTf)(3)-catalyzed process proceeds with good efficiency and with high stereoselectivity. A range of examples illustrating substrate scope are given along with a mechanistic rationale. Also demonstrated is an asymmetric cyclopropane synthesis that combines enantioselective epoxidation with this methylene-transfer protocol.
    Sprache Englisch
    Erscheinungsdatum 2009-06-10
    Erscheinungsland United States
    Dokumenttyp Journal Article
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/ja902137z
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  4. Artikel ; Online: Activation of Electron-Deficient Quinones through Hydrogen-Bond-Donor-Coupled Electron Transfer.

    Turek, Amanda K / Hardee, David J / Ullman, Andrew M / Nocera, Daniel G / Jacobsen, Eric N

    Angewandte Chemie (International ed. in English)

    2015  Band 55, Heft 2, Seite(n) 539–544

    Abstract: Quinones are important organic oxidants in a variety of synthetic and biological contexts, and they are susceptible to activation towards electron transfer through hydrogen bonding. Whereas this effect of hydrogen bond donors (HBDs) has been observed for ...

    Abstract Quinones are important organic oxidants in a variety of synthetic and biological contexts, and they are susceptible to activation towards electron transfer through hydrogen bonding. Whereas this effect of hydrogen bond donors (HBDs) has been observed for Lewis basic, weakly oxidizing quinones, comparable activation is not readily achieved when more reactive and synthetically useful electron-deficient quinones are used. We have successfully employed HBD-coupled electron transfer as a strategy to activate electron-deficient quinones. A systematic investigation of HBDs has led to the discovery that certain dicationic HBDs have an exceptionally large effect on the rate and thermodynamics of electron transfer. We further demonstrate that these HBDs can be used as catalysts in a quinone-mediated model synthetic transformation.
    Mesh-Begriff(e) Electrons ; Hydrogen Bonding ; Kinetics ; Quinones/chemistry ; Thermodynamics
    Chemische Substanzen Quinones
    Sprache Englisch
    Erscheinungsdatum 2015-11-27
    Erscheinungsland Germany
    Dokumenttyp Journal Article ; Research Support, N.I.H., Extramural ; Research Support, U.S. Gov't, Non-P.H.S.
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.201508060
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  5. Artikel ; Online: Nucleophilic acyl substitution via aromatic cation activation of carboxylic acids: rapid generation of acid chlorides under mild conditions.

    Hardee, David J / Kovalchuke, Lyudmila / Lambert, Tristan H

    Journal of the American Chemical Society

    2010  Band 132, Heft 14, Seite(n) 5002–5003

    Abstract: The first example of aromatic cation-activated nucleophilic acyl substitution has been achieved. The conversion of carboxylic acids to their corresponding acid chlorides occurs rapidly in the presence of 3,3-dichlorocyclopropenes via the intermediacy of ... ...

    Abstract The first example of aromatic cation-activated nucleophilic acyl substitution has been achieved. The conversion of carboxylic acids to their corresponding acid chlorides occurs rapidly in the presence of 3,3-dichlorocyclopropenes via the intermediacy of cyclopropenium carboxylate complexes. The effect of cyclopropene substituents on the rate of conversion is examined. The addition of tertiary amine base is found to dramatically accelerate reaction, and conditions were developed for the preparation of acid sensitive acid chlorides. Preparative scale peptide couplings of two N-Boc amino acids were achieved with this method.
    Mesh-Begriff(e) Carboxylic Acids/chemistry ; Cations/chemistry ; Hydrocarbons, Chlorinated/chemical synthesis ; Hydrocarbons, Chlorinated/chemistry ; Molecular Structure ; Stereoisomerism
    Chemische Substanzen Carboxylic Acids ; Cations ; Hydrocarbons, Chlorinated
    Sprache Englisch
    Erscheinungsdatum 2010-04-14
    Erscheinungsland United States
    Dokumenttyp Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/ja101292a
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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