Table 1.
Entry | Compound | LogP a | Retention Time (min) b | E. coli | B. subtilis | HEK-293 IC50 μg/mL | ||
---|---|---|---|---|---|---|---|---|
MIC μg/mL e | MBC μg/mL e | MIC μg/mL e | MBC μg/mL e | |||||
1 | 1a | 3.01 c | 6.1 | >2000 | >2000 | 16 | 16 | 3.2 ± 0.5 |
2 | 1b | 3.63 d | 6.2 | 128 | 256 | 4 | 8 | 0.8 ± 0.2 |
3 | 1c | 4.83 d | 7.7 | 256 | 256 | 16 | 32 | 18 ± 4 |
4 | 2a | −0.67 c | 3.4 | >2000 | >2000 | >2000 | >2000 | >45 |
5 | 2b | −0.20 d | 3.7 | >2000 | >2000 | >1000 | >1000 | >79 |
6 | 2c | −1.34 d | 3.1 | 1000 | >2000 | 128 | 256 | >142 |
7 | 3a | 3.50 c | 6.7 | 1000 | >2000 | 16 | 16 | 7.3 ± 1.2 |
8 | 3b | 4.26 d | 8.8 | 32 | 128 | 4 | 4 | 61 ± 6 |
9 | 3c | 5.96 d | 10.0 | 2000 | 2000 | 64 | 64 | 37 ± 5 |
10 | Alamethicin [41] | -- | -- | 16 | -- | 62.5 f [42] |
a Average of values calculated using VCCLab and Molinspiration software. b Retention time in HPLC C18 reverse phase, CH3CN/H2O 70/30 (0.1% HCO2H). c Value for the protonated forms. d Calculated for the imidazolium cations. e MIC/MBC values were obtained from a minimum of three separate experiments. Please refer to Supporting Information for MIC/MBC/IC 50 values in μM. f Cytotoxicity against MRC-5 cells.