Green route for the heterocyclization of 2-mercaptobenzimidazole into beta-lactum segment derivatives containing -CONH- bridge with benzimidazole: Screening in vitro antimicrobial activity with various microorganisms

Bioorg Med Chem. 2006 Dec 15;14(24):8271-9. doi: 10.1016/j.bmc.2006.09.017. Epub 2006 Oct 10.

Abstract

The efficient and rapid synthesis of novel azetidin-2-ones 4a-j has been established. Thus, both microwave and conventional condensation 2-{(1H-benzimidazol)-ylthio}-N'-2-(substituted phenyl) hydrazide with chloroacetylchloride were carried out in DMF-benzene solvent in the presence of Et(3)N catalyst. The microwave synthesis route afforded better yield with short time. The novel heterocycles were characterized by elemental analysis and spectral features. Some of the produced compounds were screened for their antimicrobial activity.

Publication types

  • Research Support, Non-U.S. Gov't

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
  • Aspergillus niger / drug effects
  • Aspergillus niger / growth & development
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology*
  • Candida / classification
  • Candida / drug effects
  • Candida / growth & development
  • Gram-Negative Bacteria / drug effects
  • Gram-Negative Bacteria / growth & development
  • Gram-Positive Bacteria / drug effects
  • Gram-Positive Bacteria / growth & development
  • Microbial Sensitivity Tests
  • Microwaves

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Benzimidazoles