Table 1.
Antiviral activity of compounds 6a–6n.
| Sr. No. | n | R1 | R2 | Heterocycle (positiona) | Dengue |
Yellow fever |
||||
|---|---|---|---|---|---|---|---|---|---|---|
| EC50 (μM) | CC50 (μM) | SI | EC50 (μM) | CC50 (μM) | SI | |||||
| 6a | 0 | F | p-methyl | D1 (ortho) | 26.5 | >116 | >4 | ND | ND | NA |
| 6b | 0 | CH3 | p-methyl | D1 (ortho) | 0.5 | >117 | >235 | ND | ND | NA |
| 6c | 0 | F | p-methyl | D2 (ortho) | 4.6 | >116 | >25 | 23 | >116 | 5 |
| 6d | 0 | CH3 | p-methyl | D2 (ortho) | 0.5 | >117 | >235 | ND | ND | NA |
| 6e | 0 | F | p-methyl | D3 (ortho) | >112 | >112 | 1 | ND | ND | NA |
| 6f | 0 | CH3 | p-methyl | D3 (ortho) | >113 | >113 | 1 | ND | ND | NA |
| 6g | 0 | F | p-methyl | D4 (ortho) | 2.1 | >116 | >55 | 10.6 | >116 | >11 |
| 6h | 0 | CH3 | p-methyl | D4 (ortho) | <0.9 | 26 | >29 | >116 | >116 | 1 |
| 6i | 1 | F | H | D4 (ortho) | 24 | 52 | 2 | 3.9 | 76 | 19 |
| 6j | 1 | CH3 | H | D4 (ortho) | >48 | 48 | 1 | 5.4 | 75 | 14 |
| 6k | 1 | F | H | D4 (para) | >116 | >116 | 1 | 18.5 | >116 | >6 |
| 6l | 1 | CH3 | H | D4 (para) | 14 | >117 | >8 | 21.5 | >117 | >5 |
| 6m | 0 | F | H | D1 (ortho) | 2.2 | >120 | >55 | 7.8 | 77 | 10 |
| 6n | 0 | CH3 | H | D1 (ortho) | 3.4 | 24 | 7 | 0.4 | >13.6 | >34 |
a
Indicates the attachment point of the heterocycle on the phenyl ring C.