Table 1. SAR Data for Synthesized Adenosine Analogues with Substitutions at Position 6a.
| ID | R or R6 | Y | Z | MtbAdoK Ki (nM) | hAdoK Ki (μM) | Mtb EC50 (μM) | HDF CC50 (μM) |
|---|---|---|---|---|---|---|---|
| 7 | R | O | N | 120.2 ± 0.9 | 5.1 ± 0.5 | ≥65.0 | 30.9 ± 4.3 |
| 8 | R | O | CH | 16.3 ± 0.1 | >50.0 | >50.0 | >50.0 |
| 9 | R | O | N | 18.5 ± 0.06 | >50.0 | >50.0 | >50.0 |
| 10 | R | O | N | 18.9 ± 0.5 | >50.0 | ≥30.0 | >50.0 |
| 11 | R6 | O | N | 19.9 ± 0.03 | >50.0 | ≥50.0 | >50.0 |
| 12 | R | O | N | 21.3 ± 0.2 | >50.0 | >50.0 | >50.0 |
| 13 | R | O | N | 23.0 ± 1.1 | ≥15.1 | >50.0 | >50.0 |
| 14 | R | O | N | 25.5 ± 2.8 | 0.41 ± 0.07 | ≥25.0 | >50.0 |
| 15 | R | CH2 | N | 27.5 ± 3.5 | >50.0 | >50.0 | >50.0 |
| 16 | R | O | N | 32.6 ± 0.3 | 1.6 ± 0.1 | >50.0 | >50.0 |
| 17 | R6 | O | N | 48.0 ± 0.6 | >50.0 | 1.7 ± 0.02 | 3.5 ± 0.4 |
| 18 | R | O | N | 5.3 ± 0.07 | >50.0 | 4.0 ± 0.2 | >50.0 |
a
The error is reported as ± SD of 2 experiments.