Synthesis and antimicrobial evaluation of 3-methanone-6-substituted- benzofuran derivatives

Jingbao Liu, Faqin Jiang, Xizhen Jiang, Wei Zhang, Jingjing Liu, Wenlu Liu, Lei Fu*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

32 Citations (Scopus)

Abstract

Seventeen benzofuran derivatives were synthesized and screened for their antibacterial activities against Escherichia coli, Staphylococcus aureus, Methicillin-resistant S. aureus, Bacillus subtilis, and Pseudomonas aeruginosa. Seven of them have showed excellent antibacterial activities compared to the positive controls (Cefotaxime and Sodium Penicillin). The substitutions at C-6 and C-3 positions of these derivatives were found to greatly impact on the antibacterial activity and strains specificity, respectively. Specifically, compounds bearing a hydroxyl group at C-6 (5a, 5b, 5c and 12) offered excellent antibacterial activities against all five above-mentioned strains (MIC 80 = 0.78-12.5 ug/mL), and those with imine (15) and (3, 4, 5-trimethoxyphenyl) methanone (7e), respectively, at C-3 position showed selective activity against S. aureus among five tested strains with great MIC80 values (3.12-12.5 ug/mL).

Original languageEnglish
Pages (from-to)879-886
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume54
DOIs
Publication statusPublished - Aug 2012
Externally publishedYes

Keywords

  • Antimicrobial
  • Benzofuran
  • Synthesis

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