One-pot two-step facile synthesis of 2,3,4,5-tetra substituted dihydrooxazoles and their antimicrobial activity

Bioorg Med Chem Lett. 2017 Aug 15;27(16):3802-3805. doi: 10.1016/j.bmcl.2017.06.062. Epub 2017 Jun 24.

Abstract

New 2,3,4,5-tetra substituted dihydrooxazoles derivatives were efficiently synthesized starting from benzaldehyde, aryl thiosemicarbazide and benzoin using designed synthetic route. Newly synthesized 2,3,4,5-tetra substituted dihydrooxazole derivatives were screened for their antibacterial and antifungal activities against different strains of pathogenic bacteria and fungi. The minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and minimum fungicidal concentration (MFC) were determined for the test compounds using positive and negative control. Compounds 4b, 4d, 4f, 4i, 4k and 4m, have shown good antibacterial activity whereas compounds 4e, 4g, 4h, 4j, 4l and 4n have displayed better antifungal activity.

Keywords: 2,3,4,5-Tetra substituted dihydrooxazoles; Antimicrobial antibacterial activity and antifungal activity; Aryl thiosemicarbazide; Benzoin; Schiff base; Thiourea.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Bacteria / drug effects*
  • Dose-Response Relationship, Drug
  • Fungi / drug effects*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Oxazoles / chemical synthesis
  • Oxazoles / chemistry
  • Oxazoles / pharmacology*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Oxazoles