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. 2014 Sep 19;57(20):8540–8562. doi: 10.1021/jm5010682

Table 2. MIC Values for Series 3 and 4.

graphic file with name jm-2014-010682_0017.jpg

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
a

Analogue 3h employs a pendant 3-pyridine in place of the pendant phenyl.