Table 3. S. aureus MICs and Cell Division Inhibitory Activity for a Set of 5-Substituted Benzothiazoles.
compd | R3 group |
S. aureus MIC (μg/mL) |
cell division inhibitiona (μg/mL) |
---|---|---|---|
6g | 5-H | 2 | 4 |
8j | 5-Cl | 0.25 | 0.25 |
8f | 5-Me | 4 | 8 |
11 | 5-propyl | 0.125 | 0.125 |
8h | 5-MeO | 2 | 2 |
8b | 5-EtO | 0.125 | 0.125 |
8a | 5-Ph | 0.25 | 0.5 |
8d | 5-Br | 0.125 | 0.25 |
8e | 5-CF3 | 0.25 | 0.5 |
18 | 5-OH | 32 | 64 |
9 | 5-NH2 | >64 | WT |
8g | 5-(dimethylamino) | >64 | WT |
16 | 5-CONH2 | >64 | WT |
14 | 5-COOH | >64 | WT |
8i | 5-COOMe | 1 | 2 |
17 | 5-(1,2,4-oxadiazol-5-yl) | 0.5 | 0.5 |
13 | 5-(imidazol-2-yl) | >64 | WT |
Lowest concentration at which ballooning of S. aureus is observed indicating on-target activity. WT: no effect on morphology.