In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
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.
Pucci
Michael J
MJ
Achillion Pharmaceuticals, 300 George Street, New Haven, CT 06511, USA. mpucci@achillion.com
Ackerman
Maria
M
Thanassi
Jane A
JA
Shoen
Carolyn M
CM
Cynamon
Michael H
MH
D000995:Antitubercular Agents / Q000737:chemistry / Q000494:pharmacology*; D027081:DNA Gyrase / Q000235:genetics / Q000378:metabolism; D024881:Drug Resistance, Bacterial; D006801:Humans; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000302:isolation & purification; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology*; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors; D014376:Tuberculosis / Q000382:microbiology
C550937:ACH 702; D000995:Antitubercular Agents; D015363:Quinolones; D013844:Thiazoles; D059005:Topoisomerase II Inhibitors; D027081:DNA Gyrase