Cleavable-complex形成由野生型和quinolone-resistant肺炎链球菌2型拓扑异构酶由gemifloxacin和其他氟喹诺酮类原料药。

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Yague G,莫里斯我,潘XS,古尔德KA,费舍尔LM

Cleavable-complex形成由野生型和quinolone-resistant肺炎链球菌2型拓扑异构酶由gemifloxacin和其他氟喹诺酮类原料药。

Antimicrob代理Chemother。2002年2月,46 (2):413 - 9。

PubMed ID

11796351 (在PubMed

]

文摘

Gemifloxacin是最近开发的氟喹诺酮类的活动对肺炎链球菌。我们表明,药物比莫西沙星更活跃,氟哌酸、左氧氟沙星、环丙沙星对肺炎链球菌菌株7785(中等收入国家,0.03到0.06 microg / ml和0.25,0.25,1和1 - 2 microg /毫升,分别)和同基因的quinolone-resistant gyrA-parC突变体(麦克风,0.5到1 microg /毫升与2到4,2到4,16岁到32岁,和64年microg /毫升,分别)。Gemifloxacin也是最有效的代理对纯化肺炎链球菌DNA促旋酶和DNA拓扑异构酶IV催化抑制和乳沟化验。药物浓度,抑制DNA成为超螺旋或DNA decatenation 50% (IC(50))是5到10和2.5到5.0 microM,分别。环丙沙星和左氧氟沙星是4到8倍不活跃与酶;莫西沙星和氟哌酸显示中间活动。drug-mediated DNA化验的乳沟促旋酶和拓扑异构酶IV,相同的效力顺序是:gemifloxacin >莫西沙星>氟哌酸>左氧氟沙星约环丙沙星。gemifloxacin,药物浓度,导致25%的线性化输入促旋酶和DNA拓扑异构酶IV 0.3 microM分别为2.5和0.1,分别;这些值是4倍,8 - 25倍低于莫西沙星,分别。每种药物诱导DNA促旋酶在同一光谱乳沟的网站但不同模式的强度。 Finally, for enzymes reconstituted with quinolone-resistant GyrA S81F or ParC S79F subunits, although cleavable-complex formation was reduced by at least 8- to 16-fold for all the quinolones tested, gemifloxacin was the most effective; e.g., it was 4- to 16-fold more active than the other drugs against toposiomerase IV with the ParC S79F mutation. It appears that the greater potency of gemifloxacin against both wild-type and quinolone-resistant S. pneumoniae strains arises from enhanced stabilization of gyrase and topoisomerase IV complexes on DNA.

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药物靶点

药物	目标	类	生物	药理作用	行动
Gemifloxacin	DNA促旋酶亚基	蛋白质	流感嗜血杆菌(写明ATCC 51907株/ DSM 11121 / KW20 / Rd)	是的	抑制剂	细节
Gemifloxacin	DNA拓扑异构酶4单元	蛋白质	流感嗜血杆菌(写明ATCC 51907株/ DSM 11121 / KW20 / Rd)	是的	抑制剂	细节