Table 5.
SAR of benzyl amide derivatives of 1 for CpIMPDH inhibition.
| ||||
|---|---|---|---|---|
| ID | X | R1 | IC50 (nM)
|
|
| (-) BSA | (+) BSA | |||
| 69 | Me | CH2Ph | > 5000 | n.d. |
| 70 | Me | Ph | 120 ± 20 | 130 ± 30 |
| 71 | (S)-Me | Ph | >5000* | n.d. |
| 72 | (R)-Me | Ph | 22.3 ± 5.9 | 28.0 ± 3.5 |
| 22 | (R)-Me | 2,3-di-ClPh | 60 ± 3 | |