Table 49.
Three-component synthesis of pyrazole-linked triazolo[1,5-a]pyrimidines 153 as anti-tubercular agents.
| |||||||
|---|---|---|---|---|---|---|---|
| Compound | R | R1 | R2 | % Inhibition at 6.25 μg/mL |
MIC (μg/mL) |
IC50 Enzyme Inhibition (μg/mL) |
CC50 VERO Cells (μg/mL) |
| 153a | H | Br | Me | 95 | 3.13 | 0.85 | 25 |
| 153b | NO2 | Br | Me | 96 | 1.56 | 0.28 | 25 |
| 153c | Cl | Br | Me | 98 | 0.78 | 0.11 | 20 |
| 153d | F | H | Me | 99 | 0.78 | 0.16 | 20 |
| 153e | F | Br | Me | 99 | 0.39 | 0.11 | 20 |
| Isoniazid a | -- | -- | -- | 99 | 0.3 | -- | -- |
| Rifampicin a | -- | -- | -- | 99 | 0.5 | -- | -- |
| Ethambutol a | -- | -- | -- | 99 | 3.12 | -- | -- |
a Reference compounds.