Table 1. In vitro activity of 5, 9, 12a–12aa against Mycobacterium tuberculosis H₃₇Rv in various assays and media and an Mtb cytochrome bd oxidase mutant cydKO.

		MIC (μM)
Entry	Compound	H37Rv MABA 2 week a	H37Rv 1 week b	H37Rv 2 week c	cydKO 2 week d
1	5	1.11	2.21	53.92	0.14
2	9	2.32	3.57	>148	0.59
3	12a	0.62	1.21	>155	0.12
4	12b	6.53	141.88	>142	0.57
5	12c	1.11	2.21	>142	0.14
6	12d	2.04	24.58	32.69	0.18
7	12e	24.58	>131	>131	3.14
8	12f	24.58	>131	>131	2.04
9	12g	2.13	4.26	>136	0.19
10	12h	>125	92.20	>125	0.37
11	12i	1.94	>125	>125	0.17
12	12j	0.56	26.35	53.25	<0.067
13	12k	3.36	103.70	>140	0.20
14	12l	0.45	0.45	>149	<0.071
15	12m	1.51	>125	>125	0.12
16	12n	0.53	0.53	24.71	<0.063
17	12o	54.22	142.69	>143	4.45
18	12p	60.90	121.80	>122	7.62
19	12q	122.00	>122	>122	90.13
20	12r	31.69	≧127	>127	3.04
21	12s	25.79	68.59	68.59	2.14
22	12t	121.55	>164	>164	41.06
23	12u	>176	>176	>176	21.98
24	12v	19.75	158.03	158.03	0.95
25	12w	>78	38.77	>155	7.13
26	12x	9.30	56.48	>74	0.45
27	12y	103.70	26.35	>140	1.09
28	12z	>125	23.42	>125	0.50
29	12aa	>128	>128	>128	>128
	PAS e	0.3	0.3	0.6	0.6
	Linezolid e	2.3	2.3	2.3	1.56
	3 e	1.56	12.5	>25	0.31

^aMIC against H₃₇Rv grown in 7H9/ADC/Tween media. MIC determination using microplate Alamar Blue assay (MABA) after 2 weeks post compound addition.

^bMIC against H₃₇Rv grown in 7H9/ADC/Tween media. MIC determination after 1 week post compound addition.

^cMIC against H₃₇Rv grown in 7H9/ADC/Tween media. MIC determination after 2 weeks post compound addition.

^dMIC against cyd knock-out strain of H₃₇Rv grown in 7H9/ADC/Tween media. MIC determination after 2 weeks post-compound addition.

^eLinezolid, PAS (p-aminosalicylic acid) and 3 were used as positive controls.