Journal
MOLECULES
Volume 20, Issue 12, Pages 22044-22057Publisher
MDPI
DOI: 10.3390/molecules201219828
Keywords
6-aminopenicillanic acid (6-APA); 2-azetidinone; beta-lactam antibiotics; antibacterial; Staudinger reaction
Funding
- Ministero dell'Istruzione, dell'Universita e dellaRicerca (MIUR)
- Centro di Tecnologie Integrate per la Salute [PONa3_00138]
- Universita di Salerno
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The synthesis and the biological activity of novel semi-synthetic -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.
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