Table 2. In vitro evaluation of the inhibitory activity and toxicity of aminopyrazoles A.1–28 a .
Compound | –R | Inhibition (%) | Toxicity (%) |
A.1 | H | <30 | 7.0 |
A.2 | 2-NO2 | 42 | 0 |
A.3 | 3-NO2 | 47 | 0 |
A.4 | 4-NO2 | 43 | 0 |
A.5 | 2-Br | 32 | 4.8 |
A.6 | 3-Br | 42 | 9.0 |
A.7 | 4-Br | 67 | >15 |
A.8 | 2-Cl | 30 | 2.4 |
A.9 | 3-Cl | <30 | 11.0 |
A.10 | 4-Cl | 56 | >15 |
A.11 | 2-F | <30 | 3.6 |
A.12 | 3-F | 48 | 0.0 |
A.13 | 4-F | <30 | 6.0 |
A.14 | 2-I | <30 | >15 |
A.15 | 3-CF3 | <30 | >15 |
A.16 | 4-CF3 | <30 | 14 |
A.17 | 2-CO2tBu | <30 | 2.8 |
A.18 | 3-CO2tBu | 36 | 0 |
A.19 | 4-CO2tBu | 47 | 14.0 |
A.20 | 2-OBn | 63 | 9.0 |
A.21 | 3-OBn | 65 | 11.0 |
A.22 | 4-OBn | <30 | 3.8 |
A.23 | 2-OMe | <30 | 9.2 |
A.24 | 3-OMe | <30 | 6.0 |
A.25 | 4-OMe | <30 | 14.6 |
A.26 | 2-C CH | <30 | 7.0 |
A.27 | 3-C CH | <30 | 14.0 |
A.28 | 4-C CH | Nd | Nd |
aData represent mean values of two experiments in duplicate.