Table 17.
Structure | R = | No. | Casp-1 IC50, nM | Casp-3 IC50, nM | Casp-8 IC50, nM | THP-1 IC50, nM | Ref |
---|---|---|---|---|---|---|---|
Reference - PRALNACASAN | |||||||
- | 77 | 3.6 | 1 300 | 40 | 190 | 286 | |
| |||||||
UNSATURATED CAPROLACTAMS | |||||||
- H | 137 | 14 | > 10000 | 2160 | 100 | 284 | |
- Me | 138 | 19 | > 10000 | 2688 | 153 | ||
- CH2OH | 139 | 22 | > 10000 | 2110 | 543 | ||
- CH2NHCOPh | 140 | 2 | 1698 | 1085 | 466 | ||
- CH2NHCO-3-OMePh | 141 | 1 | 1079 | 448 | 243 | ||
- CH2NHCO-4-OMePh | 142 | 1 | 1128 | 471 | 95 | ||
|
|||||||
MONOCYCLIC 8-MEMBERED LACTAMS | |||||||
- Ph(2-OMe) | 143 | 38 | > 10000 | > 10000 | 246 | 283 | |
- Ph(3-OMe) | 144 | 15 | > 10000 | > 10000 | 229 | ||
- Ph(3-F) | 145 | 22 | > 10000 | > 10000 | 397 | ||
- Piperonyl | 146 | 24 | > 10000 | > 10000 | 285 | ||
- N-morpholine | 147 | 44 | > 10000 | > 10000 | 224 | ||
|
|||||||
8,5-FUSED BICYCLIC PEPTIDOMIMETICS | |||||||
- Phenyl | 148 | 3.6 | 1300 | 40 | 190 | 286 | |
- 3-Chlorophenyl | 149 | 2.3 | > 10000 | 2900 | 200 | ||
- 1-Naphthyl | 150 | 1 | > 10000 | 66 | 3 | ||
- 2-Naphthyl | 151 | < 1 | > 10000 | 390 | 32 | ||
- 1-Isoquinolyl | 152 | < 1 | > 10000 | 160 | 54 | ||
|
|||||||
8,6-FUSED BICYCLIC PEPTIDOMIMETICS | |||||||
- H | 153 | 10 | > 10000 | 384 | 245 | 287 | |
- Me | 154 | 5 | > 10000 | 247 | 1820 | ||
- COPh | 155 | 7 | 8070 | 38 | 1420 | ||
- SO2Me | 156 | 6 | > 10000 | 384 | 174 | ||
- SO2Ph | 157 | 2 | > 10000 | 106 | 159 | ||
-H | 158 | 1 | > 10000 | 506 | 75 | ||
-SO2Me | 159 | 1 | > 10000 | 283 | 46 | ||
-SO2Ph | 160 | 1 | > 10000 | 50 | 153 | ||
|
|||||||
THIAZEPINES | |||||||
- Phenyl | 161 | 2 300 | > 10000 | > 10000 | 3200 | 285 | |
- 3-CF3Phenyl | 162 | - | - | - | 3400 | ||
- 2-Benzo[b]thiphene | 163 | 320 | > 10000 | 8500 | 1700 | ||
- 1-Isoquinolyl | 164 | 130 | > 10000 | 5000 | 1400 | ||
- 2-Naphthyl | 165 | 150 | > 10000 | > 10000 | 1100 | ||
|
|||||||
1-(2-ACYLHYDRAZINOCARBONYL)-CYCLOALKYL CARBOXAMIDES | |||||||
- m-Methylphenyl | 166 | 430 | - | 3120 | ≥2500 | 178 | |
- 1-Naphthyl | 167 | 40 | - | 420 | 690 | ||
- 2-Naphthyl | 168 | 30 | - | 2100 | 500 | ||
|