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. 2014 Mar 3;5(5):587–591. doi: 10.1021/ml500039g

Table 1. In Vitro Activity of the Analogues Inspired by BTZ043 against the H37Rv Strain of Mtb in 7H12 and GAS Media (MIC in μM)a.

graphic file with name ml-2014-00039g_0007.jpg

  R1 R2 MABA: 7H12 (μM) MABA: GAS (μM)
8 CF3 NO2 6.99 10.2
9 NO2 NO2 1.53 2.05
10 CF3 Br >10 nd
11 CF3 Ph >64 17.4
12 CF3 pyridine-N-oxide >64 >64
13 CF3 pyridine >50 49.3
17 CF3 H >50 17.9
18 CF3 NO2 23.0 18.4
19 NO2 NO2 47.9 22.6
23 CF3 NO2 >50 2.03
24 NO2 NO2 13.03 0.27
BTZ043     <0.02 <0.02
a

MABA, microplate alamar blue assay; GAS, glycerol-alanine-salts medium; 7H12, 7H9 medium plus casitone, palmitic acid, albumin, and catalase.