Table 2. Probing the Aromatic System on the Dipeptide N-Terminus.
compd. | R | % inhibitiona |
---|---|---|
17 | biphenyl | 77 |
18 | 4-cyclohexylphenyl | 57 |
19 | phenyl | 52 |
20 | 3,5-dichlorophenyl | 100 |
21 | meta-tert-butylphenyl | 93 |
22 | para-bromophenyl | 87 |
23 | para-chlorophenyl | 77 |
24 | meta-chlorophenyl | 79 |
25 | 3,4-diethoxyphenyl | 22 |
26 | 2,6-dichlorophenyl | 83 |
Dipeptides were evaluated at 15 μM with 20 nM BoNT/A LC and 8 μM SNAPtide substrate. Enzyme reactions were performed in triplicate, and the percent inhibition reported is the average.