Table 1. Half-Lives (t1/2) for Triazene Derivatives 11a–e and 13a–f in PBS or 80% Human Plasma at 37 °C, log P and clogP Values, and Ability to Act as Tyrosinase Substrates (100 units/mL).
|
t1/2 |
||||||
|---|---|---|---|---|---|---|
| compound | R | log P | clogPa | PBS pH 7.4 (days) | 80% human plasma (h) | tyrosinase (min) |
| 11a | Br | 3.95 ± 0.04 | 4.31 | >10 | 104.6 ± 3.2 | 0.5 ± 0.2 |
| 11b | Me | 4.21 ± 0.06 | 3.88 | >10 | 88.5 ± 0.5 | 1.9 ± 0.1 |
| 11c | CN | 3.49 ± 0.05 | 3.54 | >10 | 74.0 ± 5.6 | 0.5 ± 0.1 |
| 11d | EtOCO | 4.08 ± 0.10 | 3.88 | >10 | 30.5 ± 2.9 | 3.7 ± 0.1 |
| 11e | MeCO | 3.44 ± 0.05 | 3.51 | >10 | 61.6 ± 11.9 | 1.0 ± 0.2 |
| 13a | Br | ndb | 5.06 | 4.4 ± 0.4 | 8.3 ± 0.7 | 2.1 ± 0.1 |
| 13b | Me | nd | 4.43 | 4.2 ± 1.1 | 8.7 ± 0.4 | 2.3 ± 0.2 |
| 13c | CN | nd | 4.15 | 3.6 ± 0.2 | 2.99 ± 0.17 | nd |
| 13d | EtOCO | nd | 4.68 | 5.4 ± 0.8 | 6.57 ± 0.41 | nd |
| 13e | MeCO | nd | 3.99 | 5.8 ± 0.6 | 4.90 ± 0.33 | nd |
| 13f | Cl | nd | 4.71 | nd | nd | nd |
a
Calculated using Virtual Computational Chemistry Laboratory (VCCLAB) (http://www.vcclab.org, 2005).
b
nd: not determined.