Selected 7b-(benzo[a]dihydrocarbazolyloxyacetyl)-substituted cephalosporins (1a–e) were synthesised and tested for their antimicrobial activity against Gram-positive and Gram-negative clinical pathogens. All compounds synthesised (1a–e) showed an in vitro antimicrobial activity similar to that of ceftriaxone and cefpirome against the Gram-positive bacteria, and superior to that of penicillin and cefaclor against pen-R Staphylococcus aureus species. Like all b-lactam agents, compounds 1a–e were in an inactive Minimum Inhibitory Concentration (MIC > 32 μg/ml) against methicillin-resistant S. aureus species. Furthermore, as expected, no cross-resistance was observed against the erythromycin-resistant Staphylococcus pyogenes strain. Finally, it is worth underlining that compounds 1a and 1e showed a similar activity to that of ceftriaxone and superior to cefaclor against penicillin-resistant Streptococcus pneumoniae isolates, a key respiratory tract infection (RTI) causing pathogen difficult to treat with currently marketed antibiotics.
|Autori:||ROSSELLO ARMANDO; ORLANDINI ELISABETTA; NUTI ELISA; RAPPOSELLI SIMONA; MACCHIA MARCO; DI MODUGNO ENZA; BALSAMO A|
|Titolo:||SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF NEW 7BETA-(BENZO[A]DIHYDROCARBAZOLYLOXYACETYL)-SUBSTITUTED CEPHALOSPORINS|
|Anno del prodotto:||2004|
|Digital Object Identifier (DOI):||10.1016/j.farmac.2004.05.001|
|Appare nelle tipologie:||1.1 Articolo in rivista|