TABLE 1.

Effect of dKAA on antibacterial activity and transglycosylase inhibition by telavancin, THRX-881620, and vancomycina

dKAA concn (mM)TelavancinTHRX-881620Vancomycin
MICIC50MICIC50MICIC50
00.5 (0.3)1.2 (0.6)16 (8)90 (45)1 (0.7)10 (7)
0.54 (2)1.6 (0.8)16 (8)52 (26)256 (200)>143 (>100)
1016 (8)3 (1.5)16 (8)30 (15)>256 (>200)>143 (>100)
40NDb12 (6)ND32 (16)ND>143 (>100)
  • a Results are micrograms per milliliter with micromolar concentrations in parentheses. IC50 are the geometric means determined in a transglycosylase assay with UDP-MurNAc-pentapeptide substrate from concentration-response curves that were analyzed by nonlinear regression with a four-parameter logistic equation (Prism; GraphPad, Inc.). Each point was determined from the results from at least three separate experiments.

  • b ND, not determinable.