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. 2016 Aug 22;7(11):2122–2127. doi: 10.1039/c6md00236f

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.