TABLE 8.

Kinetic properties of selected inhibitors against different β-lactamase Ambler classesa

Inhibitor (compound no. in Fig. 1)Kinetic parameterValue (μM) for Ambler class:Reference(s)
ABCD
Aztreonam (3) Km or Ki200>1,0000.0019 56, 217, 337
BAL30072 siderophore monobactam (14)IC501.7>1000.09 134
ATMO-penicillin (15)IC500.90 418
BRL 42715 methylidene penem (16)IC500.0080.0080.004 87
BLI-489 methylidene penemIC500.0090.062 294
Novel tri- and bicyclic methylidene penems (including 17 and 18)IC500.0004-0.00310.014-0.2600.0015-0.00480.012 25, 441
LK-157 tricyclic carbapenems (20)IC500.0550.062 344
Ro 48-1220 penam sulfone (21)IC500.05-1.0724-2000.21-3.40.10-0.43 367, 422
LN-1-255 penam sulfone (23) KI or IC500.1000.0260.70 63, 322; Drawz et al., unpublished data
Boronic acid meta-carboxyphenyl cephalosporin analog (25) K i 3.90.001 272, 411
NXL104 (26)IC500.0080.080 31
J-111,225 1-β-methylcarbapenem (33) Ki 11.10.180.93 281
Phosphonates Ki 0.08-760.016-12.10.094 4, 244
C-6-mercaptomethyl penicillnate (38)IC506.80.1010.5 61
  • a The definition of KI may not be uniform from laboratory to laboratory. See the cited references for the methods used in each determination.