TABLE 4.
β-Lactamase (original host) | J-110,441
|
Hydrolysis (relative %)a
|
|||
---|---|---|---|---|---|
Hydrolysis (relative %)a | Kib(μM) | Compound 3a | Compound 7a | Imipenem | |
Metallo-β-lactamases | |||||
IMP-1 (P. aeruginosa) | 1 | 0.0037 | 2 | 2 | 100 |
CcrA (B. fragilis) | 3 | 0.23 | 22 | 18 | 100 |
L1 (S. maltophilia) | 6 | 1.00 | 61 | 40 | 100 |
Type II (B. cereus) | 8 | 0.83 | 7 | 63 | 100 |
Serine β-lactamases | |||||
Group 2b,d class A (E. coli) | <1 | 2.54 | 2 | NTc | <1 |
Group 1,d class C (E. cloacae) | <1 | 0.037 | <1 | NT | <1 |
Taking the hydrolysis rates of imipenem and cephaloridine as 100% for metallo- and serine β-lactamases, respectively.
Imipenem and cephaloridine were used as the substrates for metallo- and serine β-lactamases, respectively.
NT, not tested.
Bush’s classification (3).