Table 2. Inhibitory Activities against T. cruzi: Probing the 4-Position with Acyclic Amines.
| L | R1 | T. cruzia IC50 μM (SI) | |
|---|---|---|---|
| 14 | – | 4-Me-Ph | 0.12 (86) |
| 15 | 4-MeO-Ph | 1.2 (11) | |
| 17 | 4-F-Ph | 1.3 (38) | |
| 45 | 5-Me-pyridin-2-yl | 0.10 (<1) | |
| 46 | 6-Me-pyridin-3-yl | 31 (1.6) | |
| 47 | 2,5-Me-pyridin-3-yl | 14 (3.6) | |
| 48 | –CH2– | pyridin-2-yl | 4.4 (11) |
| 49 | pyridin-3-yl | 6.3 (8.0) | |
| 50 | 3-Me-pyridin-2-yl | 1.6 (15) | |
| 51 | 6-Me-pyridin-2-yl | 2.4 (21) | |
| 52 | –CH2CH2– | pyridin-2-yl | 3.4 (14) |
| 53 | –CH(Me)– | 2.7 (18) | |
| 54 | –CMe2– | 1.0 (25) | |
| 55 | –C(CH2CH2)– | 4.2 (12) | |
| 56 | –CH2– | 1N-Me-pyrazol-4-yl | 9.6 (5.2) |
| 57 | thiazol-2-yl | 2.7 (19) | |
| 58 | 1N-Me-imidazol-2-yl | 3.3 (14) | |
| 59 | –CH2CH2– | imidazol-1-yl | 49 (1.0) |
| 60 | – | indazol-5-yl | 6.2 (3.5) |
| 61 | pyrazolo[1,5-a]pyridin-5-yl | 11 (2.9) | |
| 62 | –CH2– | benzoxazol-2-yl | 2.5 (16) |
| 63 | –CH2CH2– | benzimidazol-1-yl | 8.2 (6.1) |
a
T. cruzi high-content infected cell assay, IC50 of total parasite count; SI = IC50/CC50 against background U2OS cell line.