Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity.
MetadataShow full item record
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.
Identifier to cite or link to this itemhttp://hdl.handle.net/10713/19640
- Synthesis and Antibacterial Activity of New Azole, Diazole and Triazole Derivatives Based on <i>p</i>-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