Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity Article Swipe
Karolina Kairytė
,
Birutė Grybaitė
,
Rita Vaickelionienė
,
Birutė Sapijanskaitė-Banevič
,
Povilas Kavaliauskas
,
Vytautas Mickevičius
·
YOU?
·
· 2022
· Open Access
·
· DOI: https://doi.org/10.3390/ph15080970
YOU?
·
· 2022
· Open Access
·
· DOI: https://doi.org/10.3390/ph15080970
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.
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- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.3390/ph15080970
- https://www.mdpi.com/1424-8247/15/8/970/pdf?version=1659786258
- OA Status
- gold
- Cited By
- 8
- References
- 39
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W4290760338
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Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W4290760338Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.3390/ph15080970Digital Object Identifier
- Title
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Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial ActivityWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2022Year of publication
- Publication date
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2022-08-06Full publication date if available
- Authors
-
Karolina Kairytė, Birutė Grybaitė, Rita Vaickelionienė, Birutė Sapijanskaitė-Banevič, Povilas Kavaliauskas, Vytautas MickevičiusList of authors in order
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https://doi.org/10.3390/ph15080970Publisher landing page
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https://www.mdpi.com/1424-8247/15/8/970/pdf?version=1659786258Direct link to full text PDF
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YesWhether a free full text is available
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-
goldOpen access status per OpenAlex
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https://www.mdpi.com/1424-8247/15/8/970/pdf?version=1659786258Direct OA link when available
- Concepts
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Antimicrobial, Chemistry, Staphylococcus aureus, Linezolid, Acetamide, Combinatorial chemistry, Hydrazone, In vitro, Multiple drug resistance, Stereochemistry, Antibiotics, Biochemistry, Biology, Bacteria, Organic chemistry, Vancomycin, GeneticsTop concepts (fields/topics) attached by OpenAlex
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8Total citation count in OpenAlex
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2025: 1, 2024: 5, 2023: 2Per-year citation counts (last 5 years)
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39Number of works referenced by this work
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10Other works algorithmically related by OpenAlex
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