Table 10. Achillion isothiazoloquinolone SAR for MRSA (MIC) and cytotoxicity in Hep2 cells.
Compound | R7 |
MRSAa
MIC (µg/ml) |
Hep2b
CC50 (µg/ml)c |
Compound | R7 |
MRSAa
MIC (µg/ml) |
Hep2b
CC50 (µg/ml)c |
---|---|---|---|---|---|---|---|
75 | 16 | >35 | 83 | 8.0 | 2 | ||
76 | 0.125 | 3 | 84 | 32 | >38 | ||
77 | 0.25 | >37 | 85 | >64 | 4 | ||
78 | 0.125 | 2 | 86 | 0.25 | 19 | ||
79 | 4.0 | 10 | 87 | 4.0 | 3 | ||
80 | 2.0 | 35 | 88 | 1.0 | >40 | ||
81 | 0.5 | 13 | 89 | 2.0 | >35 | ||
82 | 4.0 | 20 | 90 | 1.0 | 4 |
aMethicillin resistant S. aureus (methicillin- and quinolone-resistant, vancomycin intermediate-resistant; bHep2 = human laryngeal carcinoma cell line; CC50 = concentration of drug lethal to 50% of cells; 72h incubation with drug; cvalues originally reported as μM were converted to μg/ml for this table.