Al-Lahham Adnan, De Souza Noel J, Patel Mahesh, René Reinert Ralf
Institute of Medical Microbiology, National Reference Centre for Streptococci, University Hospital (RWTH Aachen), D-52057 Aachen, Germany.
J Antimicrob Chemother. 2005 Dec;56(6):1130-3. doi: 10.1093/jac/dki361. Epub 2005 Oct 20.
The new fluoroquinolones WCK 771, WCK 1152 and WCK 1153 were developed to overcome quinolone resistance in Gram-positive bacteria. The activity of these new quinolones was tested against 159 clinical isolates of Streptococcus pneumoniae and 52 clinical isolates of Streptococcus pyogenes using the microbroth dilution method.
MIC50/MIC90 values (mg/L) of WCK 771, WCK 1152 and WCK 1153 for quinolone-susceptible S. pneumoniae (n = 119; 54 penicillin G-susceptible, 53 penicillin G-intermediate, and 12 penicillin G-resistant strains) were 0.25/0.5, 0.03/0.06 and 0.016/0.03, respectively. MIC50/MIC90 values (mg/L) for quinolone-resistant pneumococci (n = 40) increased to 4/16, 0.25/1 and 0.125/0.5, respectively. Against S. pyogenes, WCK 771, WCK 1152 and WCK 1153 were also highly active with MIC50/MIC90 values (mg/L) of 0.25/0.25, 0.03/0.06 and 0.03/0.03, respectively.
Overall, WCK 771 was highly active against quinolone-susceptible, but not against quinolone-resistant S. pneumoniae, whereas WCK 1152 and WCK 1153 were more potent and were able to overcome quinolone resistance in both S. pneumoniae and S. pyogenes.
研发新型氟喹诺酮类药物WCK 771、WCK 1152和WCK 1153以克服革兰氏阳性菌对喹诺酮类药物的耐药性。采用微量肉汤稀释法检测了这些新型喹诺酮类药物对159株肺炎链球菌临床分离株和52株化脓性链球菌临床分离株的活性。
WCK 771、WCK 1152和WCK 1153对喹诺酮类敏感的肺炎链球菌(n = 119;54株对青霉素G敏感、53株对青霉素G中介、12株对青霉素G耐药菌株)的MIC50/MIC90值(mg/L)分别为0.25/0.5、0.03/0.06和0.016/0.03。对喹诺酮类耐药的肺炎球菌(n = 40)的MIC50/MIC90值(mg/L)分别增至4/16、0.25/1和0.125/0.5。对于化脓性链球菌,WCK 771、WCK 1152和WCK 1153也具有高活性,MIC50/MIC90值(mg/L)分别为0.25/0.25、0.03/0.06和0.03/0.03。
总体而言,WCK 771对喹诺酮类敏感的肺炎链球菌具有高活性,但对喹诺酮类耐药的肺炎链球菌无活性,而WCK 1152和WCK 1153活性更强,能够克服肺炎链球菌和化脓性链球菌对喹诺酮类药物的耐药性。