Table 4.
Inhibition of NOS isozymes by synthetic inhibitors
Ki (μM)* |
Selectivity |
||||
---|---|---|---|---|---|
Compounds | nNOS | eNOS | iNOS | n/e | n/i |
(±)-7 | 1.18 | 1450 | 161 | 1230 | 136 |
(±)-8 | 2.42 | 1450 | 238 | 600 | 98 |
(±)-9 | 2.3 | 1450 | 297 | 632 | 129 |
(±)-10 | 3.33 | 140 | 195 | 42 | 59 |
(±)-11 | 1.36 | 424 | 200 | 312 | 147 |
(±)-12 | 1.26 | 243 | 174 | 193 | 138 |
(±)-13 | 2.74 | 181 | 425 | 66 | 155 |
(±)-14 | 3.34 | 108 | 222 | 32 | 66 |
(±)-15 | 0.098 | 283 | 5.84 | 2890 | 60 |
(±)-16 | 0.085 | 85 | 8.95 | 1000 | 106 |
(±)-17 | 0.104 | 83 | 9.48 | 800 | 91 |
(±)-18 | 0.197 | 84 | 14.1 | 428 | 72 |
(±)-19 | 0.144 | 130 | 7.97 | 905 | 55 |
(±)-20 | 0.206 | 116 | 13.6 | 564 | 66 |
(±)-21 | 0.159 | 72 | 9.01 | 451 | 57 |
(±)-22 | 0.157 | 41 | 3.56 | 260 | 23 |
(±)-23 | 0.110 | 30 | 7.7 | 272 | 70 |
(±)-24 | 0.024 | 78 | 5.4 | 3230 | 222 |
(±)-25 | 0.027 | 18 | 4.6 | 656 | 170 |
(±)-26 | 0.014 | 28 | 4.06 | 2000 | 290 |
(±)-27 | 18.8 | 141 | 232 | 7.5 | 12 |
(±)-28 | 0.551 | 164 | 10.6 | 297 | 19 |
(±)-29 | 0.136 | 40.0 | 12.2 | 294 | 90 |
(±)-30 | 0.393 | 125 | 22.8 | 319 | 58 |
(±)-31 | 0.326 | 92.4 | 38.2 | 284 | 117 |
(±)-32 | 1.21 | 48.9 | 56.6 | 40 | 47 |
The apperent Ki values are represented as the mean from two or more independent experiments preformed in duplicate with five or six data points each and correlation coefficients of 0.89-0.99. The experimental standard deviations were less than 10%.