Table 9.
hRSV CPE Assay potency, cytotoxicity, selectivity index, and logarithmic reduction in viral plaques for analogues with structural variation in the aryl amide region of the sulfonylpyrrolidine scaffold.
| Compound No. |
 R |
EC50 (μM)a | CC50 (μM)b | SI | Virus titer log reduction |
|---|---|---|---|---|---|
| 260, ribavirin | NA | 28.4 ± 3.8 | 113.9 ± 38.5 | 3.6 | 2.5 |
| 262b | 2,4-dimethylphenyl | 2.7 ± 0.9 | 31.8 ± 7.7 | 13.1 | 1.0 |
| 262f | 2-methylphenyl | 23.8 ± 10.2 | >50 | 2.1 | NT |
| 262g | 3-methylphenyl | >50 | 25.5 ± 4.1 | 0.5 | NT |
| 262h | 4-methylphenyl | >50 | 31.7 ± 2.9 | 0.6 | NT |
| 262i | phenyl | >50 | 35.6 ± 2.3 | 0.7 | NT |
| 262j | 2-ethylphenyl | 21.2 ± 5.1 | >50 | 2.6 | NT |
| 262k | 2-i-propylphenyl | 17.6 ± 0.9 | 29.9 ± 3.5 | 1.7 | NT |
| 262l | 2,4-dimetyl-3-pyridine | >50 | >50 | 1.0 | NT |
| 262m | 3,5-dimethylphenyl | >50 | 31.3 ± 3.5 | 0.6 | NT |
| 262n | 2,4-dichlorophenyl | >50 | >50 | 1.0 | NT |
| 262o | 2,5-dimethylphenyl | 2.3 ± 0.8 | 30.9 ± 1.1 | 13.4 | 2.0 |
| 262p | 2,6-dimethylphenyl | >50 | >50 | 1.0 | NT |
| 262r | 2-methyl,5-chlorophenyl | 2.2 0.6 | 10 1.3 | 4.3 | NT |
| 262s | 2-methyl,5-trifluoromethylphenyl | >50 | 4.8 1.7 | 0.1 | NT |
| 262t | 2-methyl,5-methoxyphenyl | 4.2 ± 1.3 | 44.2 ± 5.7 | 10.4 | 1.0 |
| 262u | 2-methyl,5-i-propylphenyl | >50 | 9.7 ± 1.2 | 0.2 | NT |
| 262v | 2-methyl,5-i-butylphenyl | >50 | 6.5 ± 0.6 | 0.1 | NT |
| 262w | 2-chloro,5-methylphenyl | >50 | >50 | 1.0 | NT |
| 262x | 2-methoxy,5-methylphenyl | >50 | >50 | 1.0 | NT |
| 262y | 1-(t-butyl)-3-methyl-1H-pyrazol-5-yl | >50 | >50 | 1.0 | NT |
cNT = not tested; NA = not applicable.
a
Data are an average of ≥3 experiments.
b
Data are an average of ≥2 experiments.