Table 2.
Effects of (A) fragment 2 and its derivatives and (B) fragment 6 and a derivative on HsaD enzymic activity and growth of mycobacteria on cholesterol as carbon source
ID | Compound | Structure | IC50 (mM) | MIC (μg·mL−1) growth on cholesterol | |
---|---|---|---|---|---|
M. bovis BCG | M. tuberculosis | ||||
2 | 3,5,‐dichloro‐benzenesulfonamide |
(8). |
0.41 ± 0.02 | <12.5 | 25 |
8 | Benzenesulfonamide |
(9). |
NI | NI | NI |
24 | 3,5‐dichlorosulfanilamide |
(10). |
0.16 ± 0.01 | 25 | 200 |
27 | 3,5‐dichloro‐4‐hydroxybenzenesulphonic acid |
(11). |
0.27 ± 0.01 | >200 | >200 |
6 | ethyl 3,5‐dichloro‐4‐hydroxybenzoate |
(12). |
0.52 ± 0.02 | <12.5 | <12.5 |
32 | 3,5‐dichloro‐4‐hydroxybenzoic acid |
(13). |
0.54 ± 0.01 | <12.5 | 200 |
NI indicates no inhibition observed at 5 mM for inhibition of enzyme activity and no inhibition of growth at 200 μg·mL−1 as described in the Methods section. IC50 values shown as average ± SD (n = 6). See Supporting Information Table S1 for full list.