Table 2. Biochemical and Microbiological Activity of BLIs 18–23.
microbiological assay, MIC (μg/mL)a |
||||||||||
---|---|---|---|---|---|---|---|---|---|---|
biochemical assay, IC50 (μM)b |
K. pneumoniae |
P. aeruginosa | ||||||||
entry | clogP | tPSA | KPC-2 (class A) | AmpC (class C) | OXA-48 (class D) | VIM-2 (class B) | KPC-2 | OXA-48 | VIM-4 | VIM-2 |
18 | –1.85 | 145 | 0.019 | 0.006 | 3.14 | 2.4 | 4 | 8 | 32 | 16 |
19 | –1.99 | 128 | 0.017 | 0.01 | 7.55 | 1.4 | 2 | 2 | 0.5 | 4 |
20 | –2.39 | 134 | 0.03 | 0.032 | 0.42 | 0.02 | 0.5 | 2 | 0.5 | 0.06 |
21 | –1.32 | 111 | 0.02 | 0.003 | 1.52 | 1.5 | 4 | 16 | 32 | 16 |
22 | –2.39 | 134 | 0.03 | 0.035 | 0.67 | 0.13 | 8 | 8 | 4 | 0.5 |
23 | –1.81 | 134 | 0.022 | 0.005 | 0.288 | 0.491 | 1 | 1 | 8 | 0.5 |
Reported as the BLI concentration able to restore meropenem (fixed at 4 μg/mL) antibacterial activity.
Results are expressed as the average from duplicates unless otherwise indicated.