Table 2 In vitro cell-based screening of cyclic boronate 2.

From: Structural basis of metallo-β-lactamase, serine-β-lactamase and penicillin-binding protein inhibition by cyclic boronates

Bacterial strain

Genotype (β-lactamases)

2 MIC (μg ml1)

Meropenem MIC (μg ml1)

Meropenem MIC (μg ml 1 ) (10 μg ml 1 2)

Meropenem MIC (μg ml 1 ) (25 μg ml 1 2)

K. pneumoniae Ecl8 pSU18

bla SHV-1

>128

≤0.25

≤0.25

≤0.25

K pneumoniae Ecl8 ΔramR pSU18

bla SHV-1

>128

≤0.25

≤0.25

≤0.25

K. pneumoniae Ecl8 pSU18:NDM-1

blaSHV-1; blaNDM- 1

>128

>128

8

4

K pneumoniae Ecl8 ΔramR pSU18:NDM-1

blaSHV-1; blaNDM- 1

>128

>128

16

2

E. coli IR10

blaDHA-1; blaCTX-M-15; blaTEM-1; blaOXA-1; blaNDM- 1

>128

128

8

2

E. coli IR60

blaDHA-1; blaCTX-M-15; blaTEM-1; blaOXA-1; blaNDM- 1

>128

64

16

16

K. pneumoniae IR8

blaSHV-1; blaDHA-1; blaCTX-M-15; blaTEM-1; blaNDM-1

>128

128

32

16

  1. MIC, minimal inhibitory concentration.
  2. Testing the potency of 2 towards resenzitization of meropenem activity using well-characterized and clinically derived strains.