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.