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新型喹诺酮类药物WCK 771、WCK 1152和WCK 1153对肺炎链球菌和化脓性链球菌临床分离株的活性。

Activity of the new quinolones WCK 771, WCK 1152 and WCK 1153 against clinical isolates of Streptococcus pneumoniae and Streptococcus pyogenes.

作者信息

Al-Lahham Adnan, De Souza Noel J, Patel Mahesh, René Reinert Ralf

机构信息

Institute of Medical Microbiology, National Reference Centre for Streptococci, University Hospital (RWTH Aachen), D-52057 Aachen, Germany.

出版信息

J Antimicrob Chemother. 2005 Dec;56(6):1130-3. doi: 10.1093/jac/dki361. Epub 2005 Oct 20.

Abstract

OBJECTIVES AND METHODS

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.

RESULTS

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.

CONCLUSIONS

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.

摘要

目的与方法

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。

结果

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。

结论

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。

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