Table 1.
Cpd. | PubChem1 SID |
R1 | R2 | R3 | X | IC902 (μM) |
SI3 |
---|---|---|---|---|---|---|---|
1a | 861394 | cyclopropyl | Me | H | C-methoxy | <0.19 | >204 |
1b | 855596 | cyclopropyl | H | ethyl | CH | <0.39 | >102 |
1c | 24837296 | cyclopropyl | H | acetyl | CH | 1.6 | >26 |
1d | 855614 | ethyl | H | H | CH | 3.1 | >13 |
2a | 26660376 | 1-heptyl | 2-pyrazinyl | --- | --- | <0.19 | >12 |
2b | 26660314 | 1-hexyl | 4- methylcarboxyethylthiazol- 2-yl |
--- | --- | <0.19 | >23 |
2c | 24784170 | 3-methyl-1- butyl |
4- methylcarboxyethylthiazol- 2-yl |
--- | --- | 0.22 | 38 |
2d | 852129 | ethyl | benzimidazol-2-yl | --- | --- | 0.42 | >95 |
2e | 24807142 | 1-butyl | 5-iso-propyl-1,3,4- thiadiazol-2-yl |
--- | --- | 0.84 | >48 |
PubChem Substance Identifier; see http://pubchem.ncbi.nlm.nih.gov
Antituberculosis activity, defined as the concentration of drug inhibiting 90% growth relative to untreated controls as measured fluorometrically
Selectivity index, defined as CC50/IC90