MyJournals Home  

RSS FeedsPharmaceuticals, Vol. 15, Pages 970: Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity (Pharmaceuticals)

 
 

6 august 2022 14:05:49

 
Pharmaceuticals, Vol. 15, Pages 970: Synthesis and Biological Activity Characterization of Novel 5-Oxopyrrolidine Derivatives with Promising Anticancer and Antimicrobial Activity (Pharmaceuticals)
 


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.


 
69 viewsCategory: Medicine, Pharmacology
 
Pharmaceuticals, Vol. 15, Pages 972: Anticariogenic Activity of Three Essential Oils from Brazilian Piperaceae (Pharmaceuticals)
Pharmaceuticals, Vol. 15, Pages 973: Health Benefits and Pharmacological Aspects of Chrysoeriol (Pharmaceuticals)
 
 
blog comments powered by Disqus


MyJournals.org
The latest issues of all your favorite science journals on one page

Username:
Password:

Register | Retrieve

Search:

Pharmacology


Copyright © 2008 - 2022 Indigonet Services B.V.. Contact: Tim Hulsen. Read here our privacy notice.
Other websites of Indigonet Services B.V.: Nieuws Vacatures News Tweets Nachrichten