Table 3. Third-Round SAR Study of the C-5 Position of 4b.

| compound | R3 | FPA Inh %a |
|---|---|---|
| 3b | H | 0.9 |
| 8 | Cl | –12 |
| 9 | Br | –5 |
| 11 | CN | 1.1 |
| 12 | SCH3 | –21 |
| 13 | S(O)CH3 | 0.4 |
| 16 | S(O)2CH3 | –10 |
FPA Inh %: Fluorescence polarization inhibition rate was tested with the targeted compound at a concentration of 50 μM and the reported values were represented as the mean (n = 2).