Table 1.
Inhibition potency against MBLs, IC50, or Ki (μM).
| Inh | B1 | B2 | B3 | Ref | |||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| NDM | IMP | VIM | BcII | Other | ImiS | CphA | Sfh-I | L1 | GOB | ||
| Substrate mimic | |||||||||||
| 1 | - | 0.09 | - | - | - | - | - | - | 0.5 | - | [148] |
| 2 | - | 0.004 * | - | 0.83 * | 0.23 1,* | - | - | - | 1 * | - | [151] |
| 3 | - | - | 2 | - | 0.3 2 | - | - | - | - | - | [152] |
| 4 | - | - | - | 1.4 | - | - | - | - | 0.1 | - | [153] |
| 5a | - | 720 * | - | - | - | - | - | - | - | - | [154] |
| L-6 | 7 * | 8 * | 2.9 * | 36 * | - | - | - | 0.26 * | 12 * | 41 * | [149,150] |
| Transition state analogues | |||||||||||
| 7 | - | 213 | - | - | - | - | - | - | - | - | [156] |
| 8 | - | - | 4 * | - | - | - | 5 * | - | 0.40 * | - | [157] |
| 9 | (53) | (70) | - | Act 3 | (70) 1 | - | - | Act 4 | (70) | - | [158] |
| 10 | 0.37 | 3.88 | 1.29 | - | - | - | - | - | 1.48 | - | [159] |
| 11 | 6.06 * | - | 0.07 * | - | - | - | - | 0.72 * | - | 10.98 * | [160] |
| 12 | 631 | 126 | 316 | - | - | - | 631 | - | 336 | - | [161] |
| 13 5 | 0.01 | 2.51 | 0.0005 | - | - | - | 2.51 | - | >10 | - | [162] |
| 14 | 0.03 | 1 | 0.003 | 0.3 | 16.7 3 | - | >100 | - | N.I. | - | [147] |
| 15 | 0.032 * | 0.008 * | 0.22 * | - | - | - | - | - | N.I. | - | [163] |
| Prodrug and Irreversible inhibitors | |||||||||||
| 16 | 0.072 | 1.59 | - | - | - | 9.56 | - | - | N.I. | - | [164] |
| 17 | 2.93 | 0.28 | - | - | - | 4.86 | - | - | 6.68 | - | [165] |
| 18 | 9.44 | 0.17 | 0.66 | 0.50 | 1.32 3 | - | - | - | - | - | [166] |
| 19 | 1.31 | - | 0.19 | - | - | 3.0 | - | - | - | 0.05 | [167] |
| 20 | 16 | 12 | - | - | - | 0.02 | - | - | 0.08 | - | [168] |
| Intermediate or product mimic | |||||||||||
| L- 21 | 157 | 23 | 4.4 | 80.4 | > 500 3 | - | 950 * | - | 20 | - | [169,170,171] |
| D- 21 | 20.1 | 7.2 | 0.072 | 10.7 | 261 3 | - | 72 * | - | - | - | [169,170] |
| L epi- 21 | > 500 | 436 | 5.5 | 424 | > 500 3 | - | - | - | - | - | [169] |
| D epi- 21 | 65 | 173 | 5.5 | >500 | > 5003 | - | - | - | - | - | [169] |
| 22 | 0.7 | 0.9 | 4.6 | - | - | - | - | - | - | - | [172] |
| 23 | 2.5 | 0.3 | 4.5 | - | - | - | - | - | - | - | [172] |
| 24 | - | 0.0027 | - | - | - | - | - | - | - | - | [173] |
| 25 | 24 * | 1 * | 0.46 6,* | - | - | - | - | - | - | [174] | |
| 26 | - | - | - | - | 0.64 1,* | 7.1 * | - | - | 1.8 * | - | [175] |
| Metal displacement agents | |||||||||||
| 27 | 0.41 | 27.9 | 9.3 | - | 175 7 | - | - | - | - | - | [176,177] |
| 28 | 0.41 | 3.03 | 1.66 | - | - | - | - | - | - | - | [178] |
| 33 | 11 | (70) | 7 | - | - | - | - | - | - | - | [179,180,181] |
| 34 | 2.81 | 0.70 | 3.55 | - | - | - | - | - | - | - | [182] |
The values with an asterisk * are Ki determinations. The values between parentheses represents the inhibition percentage at the assessed concentration. 1 CcrA; 2 GIM-1; 3 SPM-1; 4 The compound activates Sfh-I; 5 additional determinations: IC50 NDM-1 0.19 μM, VIM-2 0.026 μM, and IMP-1 39.8 μM [183] and Ki NDM-1 0.081 μM, IMP-1 >30 μM, and VIM-2 0.019 μM [184]; 6 Additional determinations: Ki of 120 μM [185]; 7 DIM-1.