TABLE 1.

Inhibition of supercoiling by WT and mutant gyrase with a range of quinolones  

Compounda		Yb	Xc	IC50 (μM) for WT	Fold increase in IC50 for mutantd
No.	Name				Ala83	Ala87	Ala83 Ala87
1	Ciprofloxacin	CH	C3H5e	1.1 ± 0.23	3.0 ± 0.7	4.6 ± 0.4	38.3 ± 0.9
2	PD0117962	CF	C3H5	0.7 ± 0.06	2.7 ± 0.3	4.0 ± 0.5	29 ± 2.8
3	PD0164488	COEth	C3H5	1.7 ± 0.24	3.7 ± 0.6	4.1 ± 0.4	25 ± 0.8
4	PD0129603	CCl	C3H5	0.8 ± 0.07	2.9 ± 0.3	3.1 ± 0.6	9 ± 1.2
5	PD0163449	CBr	C3H5	0.9 ± 0.12	3.1 ± 0.2	3.5 ± 0.1	9 ± 1.3
6	Norfloxacin	CH	C2H5	4.8 ± 1.06	4.6 ± 1.0	6.6 ± 1.0	78 ± 1.8
7	Enoxacin	N	C2H5	4.4 ± 0.62	5.8 ± 1.1	15.1 ± 2.9	>2,000
8	PD0117731	CF	C2H5	2.0 ± 0.38	2.7 ± 0.1	3.6 ± 0.3	31 ± 2.1
9	Ofloxacin			3.5 ± 0.60	2.7 ± 0.1	3.1 ± 0.3	17 ± 1.0

^aCompounds 1 through 8 have structure A, while compound 9 has structure B. 

^bC-8. 

^cN-1. 

^dRelative to that for WT; calculated as IC₅₀ for mutant divided by IC₅₀ for WT. 

^eCyclopropyl form.