Table 1.
Novel Synthesized Neuronal Nitric Oxide Synthase Inhibitors with Various Selectivity and Potency on Neuronal Nitric Oxide Synthase Activity
| |
Ki (μM) |
Selectivity |
|||
|---|---|---|---|---|---|
| Compounds (cpd) | nNOS | iNOS | eNOS | nNOS/iNOS | nNOS/eNOS |
| 1 | 0.014 | 4.06 | 28 | 290 | 2000 |
| 2 | 48 | 609 | 122 | 12.7 | 2.5 |
| 3 | 0.21 | 13.6 | 116 | 64.8 | 552.4 |
| 4 | 0.088 | 18.2 | 123.9 | 207 | 1408 |
| 5 | 0.098 | 5.84 | 282.9 | 59.6 | 2886.7 |
| 6 | 0.085 | 8.95 | 85.16 | 105.3 | 1001.9 |
| 7 | 0.024 | 5.4 | 78.45 | 225 | 3268.8 |
| 8 | 0.0177 | 15 | 53.4 | 847.4 | 3017 |
nNOS/iNOS represents the selectivity of nNOS over iNOS, calculated by Ki(iNOS)/Ki(nNOS); nNOS/eNOS represents the selectivity of nNOS over eNOS, calculated by Ki(eNOS)/Ki(nNOS).
nNOS, neuronal nitric oxide synthase; iNOS, inducible NOS; eNOS, endothelial NOS.