Biological Activity, Lipophilicity and Cytotoxicity of Novel 3-Acetyl-2,5-disubstituted-1,3,4-oxadiazolines

Antibiotic resistance is now a global problem, and the lack of effective antimicrobial agents for the treatment of diseases caused by resistant microbes is increasing. The 3-acetyl-2,5-disubstituted-1,3,4-oxadiazolines presented in this article may provide a good starting point for the development of potential new effective antimicrobial agents useful in the treatment of bacterial and fungal infections. Particular attention is drawn to the 1,3,4-oxadiazole derivative marked with the number 29 with 5-nitrofuran-2-yl substituent in its chemical structure. This substance showed a strong bactericidal effect, especially against Staphylococcus spp., and no cytotoxicity to the L929 normal cell line.

Automated summary

Antibiotic resistance is a global issue with a lack of effective antimicrobial agents. The 3-acetyl-2,5-disubstituted-1,3,4-oxadiazolines may be a promising starting point for the development of new antimicrobial agents. Particularly, the 1,3,4-oxadiazole derivative with 5-nitrofuran-2-yl substituent showed strong bactericidal effect against Staphylococcus spp. and no cytotoxicity to normal cells.