TABLE 1.
Compound | IC50 (μg/ml) for topoisomerase IV wild type or with indicated alteration(s)
|
||||||
---|---|---|---|---|---|---|---|
Wild typeab | GrlAa
|
GrlBc
|
GrlA (Phe-80) and GrlB (Asn-432)c | ||||
Phe-80 | Lys-84 | Phe-80 and Lys-84 | Asn-432 | Asp-470 | |||
Levofloxacin | 2.3 | 180 | 130 | 1,160 | 14.0 ± 1.3 | 3.4 ± 0.57 | 267 ± 17 |
Ofloxacin | 3.9 | 260 | 285 | 1,250 | 41.6 ± 2.2 | 6.5 ± 2.45 | 784 ± 9.7 |
Sitafloxacin | 0.45 | 4.2 | 13 | 170 | 2.5 ± 0.33 | 0.17 ± 0.02 | 11.6 ± 0.69 |
Ciprofloxacin | 2.5 | 75 | 110 | 530 | 39.5 ± 6.3 | 4.0 ± 1.14 | 184 ± 32 |
Sparfloxacin | 7.4 | 270 | 570 | 1,190 | 59.3 ± 2.8 | 8.9 ± 0.86 | 486 ± 40 |
Tosufloxacin | 1.8 | 90 | 170 | >200 | 8.2 ± 2.1 | 1.6 ± 0.01 | 71.8 ± 19.7 |
Novobiocin | 16 | 14 | 10 | 11 | 16.4 ± 1.4 | 4.3 ± 1.86 | 24.8 ± 1.64 |
From reference 15.
For the wild type, GrlA contained Ser-80 and Glu-84 and GrlB contained Asp-432 and Asn-470.
Values are expressed as means ± standard deviations.