Table 2. MIC Values for Series 3 and 4.
compd | n | R | S. aureus MIC (μg/mL) | compd | n | R | S. aureus MIC (μg/mL) |
---|---|---|---|---|---|---|---|
3a | 2 | 3-tert-butyl | 16 | 4k | 1 | 3-CN | >256 |
3b | 2 | 2-tert-butyl | 16 | 4l | 1 | 2-CN | >256 |
3c | 2 | 4-F | 128 | 4m | 1 | 4-CF3 | >256 |
3d | 2 | 4-Cl | 32 | 4n | 1 | 3-CF3 | >256 |
3e | 2 | 4-Br | 16 | 4o | 1 | 2-CF3 | >256 |
3f | 2 | 4-CF3 | 16 | 4p | 1 | 4-F | >256 |
3g | 2 | 4-OMe | >256 | 4q | 1 | 3-F | 128 |
3h | 2 | 3-pyridyl-4-tert-butyla | 64 | 4r | 1 | 2-F | >256 |
3i | 2 | 4-NO2 | 64 | 4s | 1 | 4-OMe | 128 |
3j | 2 | 4-NH2 | >256 | 4t | 1 | 3-OMe | 128 |
3k | 2 | 4-N(CH3)2 | >256 | 4u | 1 | 2-OMe | 128 |
3l | 2 | 4-phenyl | 8 | 4v | 1 | 4-OH | 128 |
3m | 2 | 4-(4-pyridyl) | 32 | 4w | 1 | 3-OH | >256 |
3n | 2 | 4-(3-pyridyl) | 32 | 4x | 1 | 2-OH | 64 |
3o | 2 | 4-C(CH2OCH2)CH3 | >256 | 4y | 1 | 4-CO2Me | >256 |
4a | 1 | 3-tert-butyl | 32 | 4z | 1 | 3-CO2Me | >256 |
4b | 1 | 2-tert-butyl | >256 | 4aa | 1 | 2-CO2Me | >256 |
4c | 1 | 4-iso-propyl | 32 | 4cc | 1 | 4-CO2H | >256 |
4d | 1 | 4-Me | 128 | 4dd | 1 | 3-CO2H | >256 |
4e | 1 | 3-Me | 128 | 4ee | 1 | 2-CO2H | >256 |
4f | 1 | 2-Me | 128 | 4ff | 1 | 4-(3-thiophene) | 16 |
4g | 1 | 4-phenyl | 4 | 4gg | 1 | 4-(2-thiophene) | 32 |
4h | 1 | 3-phenyl | 64 | 4hh | 1 | 4-(3-furan) | 32 |
4i | 1 | 2-phenyl | >256 | 4ii | 1 | 4-(2-furan) | 32 |
4j | 1 | 4-CN | >256 | 4jj | 1 | 4-(1-pyrrole) | 32 |
Analogue 3h employs a pendant 3-pyridine in place of the pendant phenyl.