Synthesis and antimicrobial activity of new 7β-(benzo[a]dihydrocarbazolyloxyacetyl)-substituted cephalosporins
作者:Armando Rossello、Elisabetta Orlandini、Elisa Nuti、Simona Rapposelli、Marco Macchia、Enza Di Modugno、Aldo Balsamo
DOI:10.1016/j.farmac.2004.05.001
日期:2004.9
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
合成选定的7β-(苯并[a]二氢咔唑基氧基乙酰基)取代的头孢菌素(1a-e),并测试其对革兰氏阳性和革兰氏阴性临床病原体的抗菌活性。合成的所有化合物(1a-e)均显示出与头孢曲松和头孢哌酮相似的体外抗革兰氏阳性细菌的抗菌活性,并且优于青霉素和头孢克洛对金黄色葡萄球菌R-R的抗菌活性。像所有β-内酰胺类药物一样,化合物1a-e对耐甲氧西林的金黄色葡萄球菌物种的最小抑菌浓度(MIC> 32 microg / ml)不起作用。此外,如所预期的,未观察到针对耐红霉素的化脓性葡萄球菌菌株的交叉抗性。最后,