Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
Among 203 strains of Staphylococcus aureus, the MICs of CG400549 were 0.06 to 1.0 microg/ml, with MIC(50) and MIC(90) values of 0.25 microg/ml each. All strains were susceptible to linezolid and quinupristin-dalfopristin (MICs, 0.25 to 2.0 microg/ml). The daptomycin MICs were 0.25 to 2.0 microg/ml for methicillin-susceptible and 0.25 to 4.0 microg/ml against methicillin-resistant strains (including vancomycin-intermediate strains). Single-passage selection testing showed low resistance frequencies with CG400549, but multistep analysis showed that CG400549 yielded resistant mutants after 14 to 17 days in all strains tested.
Bogdanovich
Tatiana
T
Department of Pathology, Hershey Medical Center, P.O. Box 850, Hershey, PA 17033, USA.
Clark
Catherine
C
Kosowska-Shick
Klaudia
K
Dewasse
Bonifacio
B
McGhee
Pamela
P
Appelbaum
Peter C
PC
D000081:Acetamides / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D017576:Daptomycin / Q000494:pharmacology; D024901:Drug Resistance, Multiple, Bacterial / Q000235:genetics; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D000069349:Linezolid; D016106:Methicillin Resistance / Q000235:genetics; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000235:genetics; D058924:Thienopyridines; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology*; D014769:Virginiamycin / Q000494:pharmacology
D000081:Acetamides; D000900:Anti-Bacterial Agents; C523750:CG 400549; D004791:Enzyme Inhibitors; D023303:Oxazolidinones; D011725:Pyridines; D058924:Thienopyridines; D013876:Thiophenes; D014769:Virginiamycin; C062940:quinupristin-dalfopristin; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH); D000069349:Linezolid; D017576:Daptomycin