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

Int J Mol Sci. 2021 Dec 20;22(24):13669. doi: 10.3390/ijms222413669.

Abstract

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.

Keywords: N-acetyl-1,3,4-oxadiazoline derivatives; acylhydrazone; antimicrobial activity; cytotoxicity; lipophilicity.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Cell Line
  • Drug Resistance, Bacterial*
  • Humans
  • Microbial Sensitivity Tests
  • Microbial Viability / drug effects
  • Molecular Structure
  • Oxadiazoles / chemical synthesis
  • Oxadiazoles / chemistry
  • Oxadiazoles / pharmacology*
  • Staphylococcus / drug effects
  • Staphylococcus / growth & development*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Oxadiazoles