TABLE 1.

DNA supercoiling inhibition (IC₅₀s) and DNA cleavable complex formation (CC₂₅s) promoted by various fluorinated and nonfluorinated quinolones and by coumarin with wild-type or modified DNA gyrases of M. leprae

Drug	R6	IC50 (μg/ml)a				CC25 (μg/ml)
		WT	G89C	A91V	D205N	WT	G89C	A91V	D205N
Fluoroquinolones
Gatifloxacin	F	3.5	20	20	4.5	0.3	Nob	4	0.3
Moxifloxacin	F	6	30	25	6	0.8	No	12	0.7
Ofloxacin	F	15	160	80	20	9	No	110	8
Nonfluorinated quinolones
Garenoxacin	H	6	5	8	16	1	No	17	1
Nalidixic acid	H	300	150	170	600	No	No	No	No
Oxolinic acid	Bridge C6-C7	400	180	200	700	No	No	No	No
Coumarin
Novobiocin		0.25	0.3	0.2	0.3	NDc	ND	ND	ND

^aSpecific activities of 3.2 × 10³, 2.8 × 10³, 10³, 1.5 × 10³, and 3 × 10³ U/mg for wild-type (WT) GyrA, wild-type GyrB, mutant GyrA G89C, mutant GyrA A91V, and mutant GyrB D205N, respectively.

^bNo, no DNA cleavage observed.

^cND, not determined.