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In Vitro Antituberculosis Activities of ACH-702, a Novel Isothiazoloquinolone, against Quinolone-Susceptible and Quinolone-Resistant Isolates▿

机译:新型异噻唑并喹诺酮ACH-702的体外抗结核活性对喹诺酮敏感和喹诺酮抗药性分离株▿

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摘要

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 ≤1 μg/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.
机译:ACH-702是一种新型异噻唑并喹诺酮,具有针对重要细菌病原体(包括金黄色葡萄球菌)的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良好的体外抗菌活性,MIC≤1μg/ ml,与对喹诺酮敏感的菌株的氟喹诺酮莫西沙星相当,但优于对喹诺酮耐药的菌株。涉及结核分枝杆菌促旋酶的生化分析表明,与氟喹诺酮类药物相比,ACH-702具有明显改善的抑制活性。

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