新型异噻唑并喹喔啉类化合物 ACH-702 对喹诺酮类敏感和耐药分离株的体外抗结核活性。
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
机构信息
Achillion Pharmaceuticals, 300 George Street, New Haven, CT 06511, USA.
出版信息
Antimicrob Agents Chemother. 2010 Aug;54(8):3478-80. doi: 10.1128/AAC.00287-10. Epub 2010 Jun 1.
Abstract
ACH-702 is a new isothiazoloquinolone with potent in vitro and in vivo activities against important bacterial pathogens, including Staphylococcus aureus. In this study, ACH-702 was found to have promising in vitro antibacterial activity against Mycobacterium tuberculosis, with MICs of <or=1 microg/ml, comparable to that of the fluoroquinolone moxifloxacin for quinolone-susceptible isolates but superior to that for quinolone-resistant isolates. Biochemical assays involving M. tuberculosis gyrase enzymes indicated that ACH-702 had significantly improved inhibitory activity compared with fluoroquinolones.
摘要
ACH-702 是一种新型的异噻唑酮喹诺酮类药物，对包括金黄色葡萄球菌在内的重要细菌病原体具有强大的体外和体内活性。在这项研究中，发现 ACH-702 对结核分枝杆菌具有有前景的体外抗菌活性，MICs ＜或=1μg/ml，与氟喹诺酮类药物莫西沙星相当，适用于敏感的分离株，但优于耐药分离株。涉及结核分枝杆菌拓扑异构酶酶的生化测定表明，ACH-702 与氟喹诺酮类药物相比具有显著改善的抑制活性。
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