Table 22. Dainippon SAR for the C-3 position of N-1 2-thiazole quinolones: biochemical prokaryotic and eukaryotic IC50 values and cytotoxicity in a P388 murine cell line.
Scaffold | Compound | R3 |
Antibacterial activity
MIC (μg/ml) |
Cytotoxicity
CC50 (μg/ml)a |
|
---|---|---|---|---|---|
E. coli
NIHJ JC-2 |
S. aureus
209 JC-1 |
murine P388b | |||
130 | -CO2H | 0.025 | 0.39 | 0.02 | |
169 | -H | 12.5 | 12.5 | 0.18 | |
170 | -CONH2 | >100 | >100 | 0.27 | |
11 | -CO2H vosaroxin |
1.56 | 3.13 | 0.01 | |
171 | -CH2OH | >100 | 25 | 0.06 |
a Concentration that reduces cell viability by 50%; bmurine lymphocytic leukaemia cell line.