Synthesis and antimicrobial activity of new 7 beta-(benzo[a]dihydrocarbazolyloxyacetyl)-substituted cephalosporins.
Selected 7beta-(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 beta-lactam agents, compounds 1a-e were in an inactive Minimum Inhibitory Concentration (MIC > 32 microg/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.
Rossello
Armando
A
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Pisa, via Bonanno, 6, Pisa 56126, Italy. aros@farm.unipi.it
Orlandini
Elisabetta
E
Nuti
Elisa
E
Rapposelli
Simona
S
Macchia
Marco
M
Di Modugno
Enza
E
Balsamo
Aldo
A
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D013210:Staphylococcus / Q000187:drug effects / Q000254:growth & development
D000900:Anti-Bacterial Agents; D002511:Cephalosporins