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Molecules 2015, 20(12), 22044-22057; doi:10.3390/molecules201219828

Novel Penicillin-Type Analogues Bearing a Variable Substituted 2-Azetidinone Ring at Position 6: Synthesis and Biological Evaluation

1
Dipartimento di Chimica e Biologia, Università degli Studi di Salerno, via Giovanni Paolo II, 132, Fisciano 84084, Italy
2
S.S.D. “Sperimentazione Animale”, National Cancer Institute, I.R.C.C.S. “Fondazione Pascale”, Naples 80131, Italy
3
Dipartimento di Farmacia, Università degli Studi di Salerno, via Giovanni Paolo II, 132, Fisciano 84084, Italy
*
Authors to whom correspondence should be addressed.
Academic Editor: Peter J. Rutledge
Received: 28 September 2015 / Revised: 20 November 2015 / Accepted: 2 December 2015 / Published: 10 December 2015
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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. View Full-Text
Keywords: 6-aminopenicillanic acid (6-APA); 2-azetidinone; β-lactam antibiotics; antibacterial; Staudinger reaction 6-aminopenicillanic acid (6-APA); 2-azetidinone; β-lactam antibiotics; antibacterial; Staudinger reaction
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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De Rosa, M.; Vigliotta, G.; Palma, G.; Saturnino, C.; Soriente, A. Novel Penicillin-Type Analogues Bearing a Variable Substituted 2-Azetidinone Ring at Position 6: Synthesis and Biological Evaluation. Molecules 2015, 20, 22044-22057.

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