Synthesis and biological activity of novel series of 1,3-benzoxazol-2(3H)-one derivatives

Acta Pol Pharm. 2013 Mar-Apr;70(2):245-53.

Abstract

In the search for novel biological agents, a series of new derivatives N-substituted 1,3-benzoxazol-2(3H)-one, 5-chloro-1,3-benzoxazol-2(3H)-one, 6-bromo-1,3-benzoxazol-2(3H)-one were prepared. All of the compounds were characterized by 1H NMR, 13C NMR and ESI MS spectra. Moreover, for compound 1 an Xray structure was determined. All derivatives were tested for antimicrobial activity against a selection of Gram-positive, Gram-negative bacteria and yeasts. The selected compounds (2-8, 10) were tested for their cytotoxic properties in K562, HeLa and normal cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Benzoxazoles / chemical synthesis*
  • Benzoxazoles / pharmacology*
  • Cell Survival / drug effects
  • Crystallography, X-Ray
  • Dose-Response Relationship, Drug
  • Gram-Negative Bacteria / drug effects
  • Gram-Negative Bacteria / growth & development
  • HeLa Cells
  • Human Umbilical Vein Endothelial Cells / drug effects
  • Humans
  • Inhibitory Concentration 50
  • K562 Cells
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Spectrometry, Mass, Electrospray Ionization
  • Structure-Activity Relationship
  • Yeasts / drug effects
  • Yeasts / growth & development

Substances

  • Anti-Infective Agents
  • Antineoplastic Agents
  • Benzoxazoles
  • benzoxazolone