Synthesis and antimicrobial activity of new 7β-(benzo[a]dihydrocarbazolyloxyacetyl)-substituted cephalosporins
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- 作者：Rossello ; Armando ; Orlandini ; Elisabetta ; Nuti ; Elisa ; Rapposelli ; Simona ; Macchia ; Marco ; et. al.
- 关键词：Cephalosporins ; 7β ; -(benzo[a]dihydrocarbazolyloxyacetyl)-substituted ; Antimicrobial activity
- 刊名：Il Farmaco
- 出版年：2004
- 出版时间：September, 2004
- 年：2004
- 卷：59
- 期：9
- 页码：691-696
- 全文大小：243 K
文摘
Selected 7β-(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 β-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.