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

6533b854fe1ef96bd12af55c

RESEARCH PRODUCT

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

Carmela Saturnino Giuseppe Palma Margherita De Rosa Giovanni Vigliotta Annunziata Soriente

subject

Salmonella typhimurium Cell Survival medicine.drug_class Stereochemistry Staphylococcus Gram-positive bacteria Antibiotics Penicillanic Acid Pharmaceutical Science Bacillus 6-aminopenicillanic acid (6-APA); 2-azetidinone; β-lactam antibiotics; antibacterial; Staudinger reaction Microbial Sensitivity Tests beta-Lactams medicine.disease_cause Article 6-aminopenicillanic acid (6-APA)Analytical Chemistry lcsh:QD241-441 Mice Structure-Activity Relationship lcsh:Organic chemistry Staphylococcus epidermidis Pseudomonas β-lactam antibiotics Drug Discovery Escherichia coli medicine Animals Physical and Theoretical Chemistry biology Chemistry Organic Chemistry Biological activity biology.organism_classification Antimicrobial Anti-Bacterial Agents Penicillin antibacterial Chemistry (miscellaneous)Staphylococcus aureus NIH 3T3 Cells 2-azetidinone Azetidines Molecular Medicine Staudinger reaction Bacteria medicine.drug

description

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.

year	journal	country	edition	language
2015-12-10	Molecules

10.3390/molecules201219828 http://dx.doi.org/10.3390/molecules201219828

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