Novel penicillin-type analogues bearing a variable substituted 2-azetidinone ring at position 6: Synthesis and biological evaluation

Margherita De Rosa, Giovanni Vigliotta, Giuseppe Palma, Carmela Saturnino, Annunziata Soriente

Research output: Contribution to journalArticlepeer-review

Abstract

The synthesis and the biological activity of novel semi-synthetic β-Lactam compounds containing an azetidinone moiety joined to the amino-nitrogen of the (+)-6-aminopenicillanic acid (6-APA) as new antibacterial agents is reported. The synthesized compounds were screened for their in vitro antimicrobial activity against a panel of Gram positive and Gram negative pathogens and environmental bacteria. Tested compounds displayed good antimicrobial activity against all tested Gram positive bacteria and for Staphylococcus aureus and Staphylococcus epidermidis antimicrobial activity resulted higher than that of the reference antibiotic. Additionally, in vitro cytotoxic screening was also carried out indicating that the compounds do not cause a cell vitality reduction effective at concentration next to and above those shown to be antimicrobial.

Original languageEnglish
Pages (from-to)22044-22057
Number of pages14
JournalMolecules
Volume20
Issue number12
DOIs
Publication statusPublished - Dec 10 2015

Keywords

  • 2-azetidinone
  • 6-aminopenicillanic acid (6-APA)
  • Antibacterial
  • Staudinger reaction
  • βtam antibiotics

ASJC Scopus subject areas

  • Organic Chemistry

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