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dc.contributor.authorKairytė, Karolina
dc.contributor.authorGrybaitė, Birutė
dc.contributor.authorVaickelionienė, Rita
dc.contributor.authorSapijanskaitė-Banevič, Birutė
dc.contributor.authorKavaliauskas, Povilas
dc.contributor.authorMickevičius, Vytautas
dc.date.accessioned2022-08-30T13:39:02Z
dc.date.available2022-08-30T13:39:02Z
dc.date.issued2022-08-06
dc.identifier.urihttp://hdl.handle.net/10713/19640
dc.description.abstractThe 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.en_US
dc.description.urihttps://doi.org/10.3390/ph15080970en_US
dc.language.isoenen_US
dc.publisherMDPIen_US
dc.relation.ispartofPharmaceuticalsen_US
dc.subjectA549en_US
dc.subjectMRSAen_US
dc.subjectStaphylococcus aureusen_US
dc.subjectantimicrobial propertiesen_US
dc.subjectazoleen_US
dc.subjectbiological activityen_US
dc.subjectbishydrazoneen_US
dc.subjecthydrazoneen_US
dc.subjectlung canceren_US
dc.subjectmultidrug-resistant pathogensen_US
dc.subjectpyrrolidinoneen_US
dc.titleSynthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity.en_US
dc.typeArticleen_US
dc.identifier.doi10.3390/ph15080970
dc.identifier.pmid36015119
dc.source.journaltitlePharmaceuticals (Basel, Switzerland)
dc.source.volume15
dc.source.issue8
dc.source.countrySwitzerland


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