Table 1.
Compd | R1 | pIC50 [a] | |||
---|---|---|---|---|---|
4‐ | 3‐ | 2‐ | T. cruzi | MRC‐5 | |
3 | Br | H | H | 5.4 | <4.2 |
7 a | H | Br | H | <4.2 | <4.2 |
7 b | H | H | Br | <4.2 | <4.2 |
7 c | H | H | H | <4.2 | <4.2 |
7 d | Cl | H | H | 5.3 | 5.1 |
7 e | H | Cl | H | <4.2 | <4.2 |
7 f | H | H | Cl | <4.2 | <4.2 |
7 g | F | H | H | <4.2 | <4.2 |
7 h | H | F | H | 5.2 | 4.4 |
7 i | H | H | F | 4.3 | <4.2 |
7 j | OMe | H | H | 5.0 | <4.2 |
7 k | H | OMe | H | 5.1 | 4.4 |
7 l | H | H | OMe | <4.2 | <4.2 |
7 m | NMe2 | H | H | <4.2 | <4.2 |
7 n | H | NMe2 | H | <4.2 | <4.2 |
7 o | CN | H | H | <4.2 | <4.2 |
7 p | H | CN | H | <4.2 | <4.2 |
7 q | OMe | F | H | 5.2 | <4.2 |
7 r | OMe | Cl | H | 5.9 | <4.2 |
7 s | OMe | Br | H | 6.4 | <4.2 |
7 t | Cl | OMe | H | <4.2 | <4.2 |
7 u | Br | OMe | H | <4.2 | <4.2 |
7 v | OMe | OMe | H | 4.3 | <4.2 |
7 w | F | F | H | 5.1 | <4.2 |
[a] All reported values are within a standard deviation of ±0.2.