TABLE 5.
Kinetic constants (k chem and k 2nd) of the selected compound set investigated by the cysteine reactivity assay. Selectivity indices were calculated from k 2nd/k chem.
| Cpd. | Structure | Cysteine k chem (M−1min−1) | SrtA k 2nd (M−1min−1) | S. I. |
|---|---|---|---|---|
| 5a |
|
50.8 ± 16.6 | 8,088 ± 464 | 159 |
| 5c |
|
63.0 ± 2.01 | 0 | — |
| 6a |
|
63.3 ± 8.37 | 20,785 ± 4,074 | 327 |
| 6i |
|
0 | 0 | — |
| 7a |
|
104.9 ± 22.5 | 28,185 ± 2,117 | 268 |
| 7b |
|
104.1 ± 19.4 | 13,998 ± 1,462 | 134 |
| 7c |
|
33.58 ± 2.93 | 4,364 ± 596 | 129 |
| 7d |
|
6.14 ± 1.71 | 1,204 ± 139 | 196 |
| 7e |
|
0 | 0 | — |