Singh K V, Coque T M, Murray B E
Department of Internal Medicine, University of Texas Medical School, Houston 77030, USA.
Antimicrob Agents Chemother. 1996 Sep;40(9):2142-6. doi: 10.1128/AAC.40.9.2142.
The in vitro activity of the trinem sanfetrinem (formerly GV104326) (GV) was compared with that of vancomycin, ampicillin, and/or nafcillin against 287 gram-positive bacteria, including methicillin-resistant Staphylococcus aureus and multiresistant enterococci, by the agar and microbroth dilution methods. GV demonstrated 2 to 16 times more activity than ampicillin and nafcillin against the majority of these organisms. The MIC range of GV was 16 to 64 micrograms/ml for 19 Enterococcus faecium strains that were highly resistant to ampicillin (ampicillin MIC range, 64 to 512 micrograms/ml) and vancomycin resistant and 0.25 to 32 micrograms/ml for resistant Rhodococcus spp. Similar activities (+/-1 dilution) were observed by either the agar or the broth microdilution method. GV demonstrated bactericidal activity against a beta-lactamase-producing Enterococcus faecalis strain and against two methicillin-susceptible Staphylococcus aureus strains in 10(5)-CFU/ml inocula. Synergy between GV and gentamicin was observed against an E. faecalis strain that lacked high-level gentamicin resistance. The activity of GV suggests this compound warrants further study.
采用琼脂稀释法和微量肉汤稀释法,将三嗪类药物三苯沙林(以前称为GV104326,简称GV)的体外活性与万古霉素、氨苄西林和/或萘夫西林针对287株革兰氏阳性菌(包括耐甲氧西林金黄色葡萄球菌和多重耐药肠球菌)的活性进行了比较。针对这些微生物中的大多数,GV的活性比氨苄西林和萘夫西林高2至16倍。对于19株对氨苄西林高度耐药(氨苄西林MIC范围为64至512微克/毫升)且耐万古霉素的屎肠球菌菌株,GV的MIC范围为16至64微克/毫升,对于耐药红球菌属,GV的MIC范围为0.25至32微克/毫升。通过琼脂稀释法或肉汤微量稀释法观察到相似的活性(±1个稀释度)。在接种量为10(5)CFU/毫升时,GV对一株产β-内酰胺酶的粪肠球菌菌株和两株甲氧西林敏感的金黄色葡萄球菌菌株具有杀菌活性。在一株缺乏高水平庆大霉素耐药性的粪肠球菌菌株中,观察到GV与庆大霉素之间具有协同作用。GV的活性表明该化合物值得进一步研究。