• Login
    View Item 
    •   UMB Digital Archive
    • UMB Open Access Articles
    • UMB Open Access Articles
    • View Item
    •   UMB Digital Archive
    • UMB Open Access Articles
    • UMB Open Access Articles
    • View Item
    JavaScript is disabled for your browser. Some features of this site may not work without it.

    Browse

    All of UMB Digital ArchiveCommunitiesPublication DateAuthorsTitlesSubjectsThis CollectionPublication DateAuthorsTitlesSubjects

    My Account

    LoginRegister

    Statistics

    Display statistics

    Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity.

    • CSV
    • RefMan
    • EndNote
    • BibTex
    • RefWorks
    Author
    Kairytė, Karolina
    Grybaitė, Birutė
    Vaickelionienė, Rita
    Sapijanskaitė-Banevič, Birutė
    Kavaliauskas, Povilas
    Mickevičius, Vytautas
    Date
    2022-08-06
    Journal
    Pharmaceuticals
    Publisher
    MDPI
    Type
    Article
    
    Metadata
    Show full item record
    See at
    https://doi.org/10.3390/ph15080970
    Abstract
    The 1-(4-acetamidophenyl)-5-oxopyrrolidine carboxylic acid was applied for synthesizing derivatives bearing azole, diazole, and hydrazone moieties in the molecule. Modification of an acetamide fragment to the free amino group afforded compounds with two functional groups, which enabled to provide a series of 4-substituted-1-(4-substituted phenyl)pyrrolidine-2-ones. The resulted compounds 2 and 4-22 were subjected to the in vitro anticancer and antimicrobial activity determination. The compounds 18-22 exerted the most potent anticancer activity against A549 cells. Furthermore, compound 21 bearing 5-nitrothiophene substituents demonstrated promising and selective antimicrobial activity against multidrug-resistant Staphylococcus aureus strains, including linezolid and tedizolid-resistant S. aureus. These results demonstrate that 5-oxopyrolidine derivatives are attractive scaffolds for the further development of anticancer and antimicrobial compounds targeting multidrug-resistant Gram-positive pathogens.
    Keyword
    A549
    MRSA
    Staphylococcus aureus
    antimicrobial properties
    azole
    biological activity
    bishydrazone
    hydrazone
    lung cancer
    multidrug-resistant pathogens
    pyrrolidinone
    Show allShow less
    Identifier to cite or link to this item
    http://hdl.handle.net/10713/19640
    ae974a485f413a2113503eed53cd6c53
    10.3390/ph15080970
    Scopus Count
    Collections
    UMB Open Access Articles

    entitlement

    Related articles

    • Synthesis and Antibacterial Activity of New Azole, Diazole and Triazole Derivatives Based on p-Aminobenzoic Acid.
    • Authors: Sapijanskaitė-Banevič B, Palskys V, Vaickelionienė R, Šiugždaitė J, Kavaliauskas P, Grybaitė B, Mickevičius V
    • Issue date: 2021 Apr 29
    • Synthesis of Novel Thiazole Derivatives Bearing β-Amino Acid and Aromatic Moieties as Promising Scaffolds for the Development of New Antibacterial and Antifungal Candidates Targeting Multidrug-Resistant Pathogens.
    • Authors: Malūkaitė D, Grybaitė B, Vaickelionienė R, Vaickelionis G, Sapijanskaitė-Banevič B, Kavaliauskas P, Mickevičius V
    • Issue date: 2021 Dec 23
    • Tedizolid: a novel oxazolidinone with potent activity against multidrug-resistant gram-positive pathogens.
    • Authors: Zhanel GG, Love R, Adam H, Golden A, Zelenitsky S, Schweizer F, Gorityala B, Lagacé-Wiens PR, Rubinstein E, Walkty A, Gin AS, Gilmour M, Hoban DJ, Lynch JP 3rd, Karlowsky JA
    • Issue date: 2015 Feb
    • Synthesis, characterization and evaluation of 1,3,5-triazine aminobenzoic acid derivatives for their antimicrobial activity.
    • Authors: Al-Zaydi KM, Khalil HH, El-Faham A, Khattab SN
    • Issue date: 2017 May 10
    • [Pharmacological action and clinical effect of tedizolid phosphate (SIVEXTRO(®) Tablets 200 mg, for iv infusion 200 mg), a novel oxazolidinone-class antibacterial drug].
    • Authors: Mori M, Takase A
    • Issue date: 2020
    DSpace software (copyright © 2002 - 2023)  DuraSpace
    Quick Guide | Policies | Contact Us | UMB Health Sciences & Human Services Library
    Open Repository is a service operated by 
    Atmire NV
     

    Export search results

    The export option will allow you to export the current search results of the entered query to a file. Different formats are available for download. To export the items, click on the button corresponding with the preferred download format.

    By default, clicking on the export buttons will result in a download of the allowed maximum amount of items.

    To select a subset of the search results, click "Selective Export" button and make a selection of the items you want to export. The amount of items that can be exported at once is similarly restricted as the full export.

    After making a selection, click one of the export format buttons. The amount of items that will be exported is indicated in the bubble next to export format.