Table 8.
5- and 7-Substituted Quinolinones
|
||||
|---|---|---|---|---|
| compound | R1 | R2 | MIC (μg/mL) | clog P |
| 111 | CF3 | 5-(trifluoromethyl)pyridin-2-yl-amino | <0.0625 | 3.8 |
| 112 | CF3 | 3,4-dichloroanilino | <0.0625 | 5.2 |
| 113 | CF3 | 3,4-difluoroanilino | <0.0625 | 4.1 |
| 114 | CF3 | 5-(fluoro)pyridin-2-yl-amino | 0.125 | 3.1 |
| 115 | CF3 | 6-(trifluoromethyl)pyridazine-3-yl-amino | 1 | 2.9 |
| 116 | CF3 | 5-dimethylaminopyridin-2-yl-amino | 2 | 3.6 |
| 117 | CF3 | (N,N-dimethyl-6-sulfamoyl) pyridin-2-yl-amino | 2 | 2.1 |
| 118 | CF3 | 1H-indazol-4-yl-amino | 2 | 3.6 |
| 119 | CF3 | morpholino | >32 | 2.1 |
| 120 | CF3 | 4-(trifluoromethyl)cyclohexyl-amino | 0.125 | 3.9 |
| 122 | F | 5-(trifluoromethyl)pyridin-2-yl-amino | 1 | 3.1 |