Table 3. Inhibitory Activity of Benzothiazole Compounds with Neutral or Basic Terminal Functional Groups.

		IC50 (nM) or RA (%)a
Cmpd	R	E. coli gyrase	E. coli topo IV	S. aureus gyrase	S. aureus topo IV
9c		66 ± 8 nM	100%	35 400 nM	100%
12		16 000 ± 4 000 nM	100%	60%	100%
15a	-CH3	9.5 ± 2.5 nM	4 600 ± 100 nM	400 ± 120 nM	1 600 ± 300 nM
15b	-NH2	26 ± 8 nM	5 200 ± 2 700 nM	1 300 ± 600 nM	5 800 ± 3 100 nM
15c	-pyridine-4-yl	2 500 ± 1 500 nM	100%	100%	100%
15d	-CH2CH2NHBoc	110 ± 20 nM	100%	780 nM	100%
15e	-CH2NHBoc	29 ± 15 nM	60%	260 ± 120 nM	100%
16a	-CH2CH2NH3+Cl–	110 ± 50 nM	10 000 ± 2 000 nM	1 500 ± 600 nM	290 ± 180 nM
16b	-CH2NH3+Cl–	280 ± 10 nM	100%	380 nM	100%

^aResidual activity of the enzyme at 10 μM concentration of the compound.