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