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.