Table 2: Half-lives (t1/2) of triazene
derivatives (18a-18f) in PBS buffer, 80% human plasma and in
the presence of tyrosinase (300 U/mL) at 37șC.
Compound
|
X |
t1/2 |
||
7.4 buffer (h) |
80% human lasma (h) |
Tyrosinase (min) |
||
18a |
COMe |
56.6 ± 1.0 |
1.41 ± 0.13 |
19.9 ± 1.2 |
18b |
CO2Et |
70.3 ± 0.8 |
5.32 ± 0.08 |
18.0 ± 1.2 |
18c |
CN |
42.7 ± 0.5 |
1.23 ± 0.17 |
15.6 ± 1.8 |
18d |
Br |
a |
6.80 ±
0.01 |
8.9 ± 0.10 |
18e |
CONH2 |
40.6 ± 0.6 |
5.19 ± 0.08 |
17.4 ± 0.42 |
18f |
CO2Me |
75.1 ±
1.7 |
2.80 ± 0.26 |
18.3 ± 0.56 |
Substrate
concentration 10-5 M.
aStable for 15 days.