Table 2.
Inhibition of human NOS enzymes by 1,6-disubstituted indole derivatives
| |||||||
|---|---|---|---|---|---|---|---|
| Compound | X | R | nNOS IC50 a (μM) | eNOS IC50 a (μM) | iNOS IC50 a (μM) | eNOS/nNOS | iNOS/nNOS |
| 32 | S |
|
1.4 (1.1–1.6) | 17.1 (11.4–24.7) | 70 (31.8–155) | 12.1 | 50 |
| 33 | O |
|
1.0 (0.68–1.4) | 19.1 (15.9–24.7) | >100b | 19 | NCc |
Values reported in parentheses are 95% confidence intervals.
a
Inhibitory activities were measured by the conversion of [3H]-L-arginine into [3H]-L-citrulline.
b
Not active at the maximum test concentration of 100 μM.
c
Not calculable.