Table 3. Second-Generation Dipeptides.
| compd. | AA1 | AA2 | R | IC50 (μM)a |
|---|---|---|---|---|
| 27 | Nva | Ile | biphenyl-4-chloro | 1.0 |
| 2 | Ile | Phe | biphenyl-4-chloro | 2.4 |
| 28 | Ile | Val | biphenyl-4-chloro | 2.9 |
| 20 | Ile | Phe | 3,5-dichlorophenyl | 0.15 |
| 29 | Leu | Ile | 3,5-dichlorophenyl | 0.15 |
| 30 | Nva | Ile | 3,5-dichlorophenyl | 0.089 |
| 31 | Ile | Val | 3,5-dichlorophenyl | 0.069 |
| 32 | Nva | Phe | 3,5-dichlorophenyl | 0.043 |
| 33 | Val | Phe | 3,5-dichlorophenyl | 0.021 |
Dipeptides were evaluated using 20 nM BoNT/A LC, 8 μM SNAPtide substrate, and a range of dipeptide concentrations to determine IC50 values.
