In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.

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.

• Authors: Michael J Pucci, Maria Ackerman, Jane A Thanassi, Carolyn M Shoen, Michael H Cynamon
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 54 Issue 8 Pg. 3478-80 (Aug 2010) ISSN: 1098-6596 [Electronic] United States
• PMID: 20516287 (Publication Type: Journal Article)

Chemical References

• ACH 702
• Antitubercular Agents
• Quinolones
• Thiazoles
• Topoisomerase II Inhibitors
• DNA Gyrase

Topics

• Antitubercular Agents (chemistry, pharmacology)
• DNA Gyrase (genetics, metabolism)
• Drug Resistance, Bacterial
• Humans
• Microbial Sensitivity Tests
• Mycobacterium tuberculosis (drug effects, isolation & purification)
• Quinolones (chemistry, pharmacology)
• Thiazoles (chemistry, pharmacology)
• Topoisomerase II Inhibitors
• Tuberculosis (microbiology)