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. 2010 Apr 28;53(10):3927–3936. doi: 10.1021/jm9016366

Table 3. S. aureus MICs and Cell Division Inhibitory Activity for a Set of 5-Substituted Benzothiazoles.

graphic file with name jm-2009-016366_0002.jpg

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
a

Lowest concentration at which ballooning of S. aureus is observed indicating on-target activity. WT: no effect on morphology.