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. 2018 Mar 22;9(4):359–364. doi: 10.1021/acsmedchemlett.7b00548

Table 1. Inhibitory Activity (IC50, μM) of Rhodanines against Four MβLs in 50 mM Tris-HCl, pH 7.0a.

  B1
B2 B3   B1
B2 B3
compd NDM-1b VIM-2b ImiSc L1b compd NDM-1b VIM-2b ImiSc L1b
1a       0.32 ± 0.02 2b 0.69 ± 0.02     0.18 ± 0.02
1b 47 ± 1     1.7 ± 0.1 2c 14.3 ± 0.4     0.59 ± 0.02
1c       0.77 ± 0.09 2d 1.13 ± 0.06 0.92 ± 0.02   0.21 ± 0.02
1d     19.1 ± 0.6 0.16 ± 0.03 2e   1.9 ± 0.3 16.5 ± 0.3 0.12 ± 0.01
1e       0.37 ± 0.01 2f     6.9 ± 0.2 0.10 ± 0.01
1f   27.9 ± 0.3   0.28 ± 0.01 2g 12 ± 1   15.0 ± 0.3 0.31 ± 0.02
1g 25.1 ± 0.8     0.6 ± 0.1 2h 12.2 ± 0.9 3.6 ± 0.1 7.7 ± 0.9 0.070 ± 0.002
1h   15.3 ± 0.8   0.22 ± 0.06 2i 10.6 ± 0.8 3.5 ± 0.2 7.6 ± 0.2 0.030 ± 0.008
1i 21.5 ± 0.8 25.1 ± 0.4   0.080 ± 0.002 2j 8.4 ± 0.4 6.9 ± 0.2 3.6 ± 0.1 0.080 ± 0.003
1j 15.4 ± 0.9 14.4 ± 0.6   0.20 ± 0.02 2k 10.6 ± 0.5 2.36 ± 0.09 7.8 ± 0.5 0.070 ± 0.008
1k 14.3 ± 0.9 12.7 ± 0.9   0.11 ± 0.02 2l 1.31 ± 0.05 0.19 ± 0.03 3.0 ± 0.2 0.050 ± 0.003
1l 27.4 ± 0.4 16.8 ± 0.4   0.22 ± 0.01 2m 6.7 ± 0.2 3.9 ± 0.3 15.9 ± 0.8 0.020 ± 0.004
1m       0.10 ± 0.01 3a   4.7 ± 0.4   0.32 ± 0.01
2a 8.7 ± 0.9   18.3 ± 0.2 0.21 ± 0.01          
a

Blank spaces represent percent inhibition under 50% at a concentration of 50 μM.

b

The antibiotic used was cefazolin.

c

The antibiotics used was imipenem.