Table 2.
M. tuberculosis H37Rv | M. abscessus ATCC 19977 | M. smegmatisa | ||||||
---|---|---|---|---|---|---|---|---|
Compound | WT MIC (µg ml−1) | ∆1258c MIC (µg ml−1) | Efflux Ratio | WT MIC (µg ml−1) | ∆2780c MIC (µg ml−1) | Efflux Ratio | WT MIC (µg ml-1) | Ribo. IC50 (µM) |
SPC (1) | 64 | 4 | 16 | 512 | 16 | 32 | 64 | 0.80b |
TroSPC (2) | 32 | 2 | 16 | 64 | 16 | 4 | 32 | 0.51 |
SPA (3) | 2 | 4 | 0.5 | 64c | 16c | 4c | ND | 1.80d |
TroSPA (4) | 2 | 1 | 2 | 64 | 16 | 4 | 32 | 2.45 |
bAmSPC (5) | 16 | 2 | 8 | 128 | 8 | 16 | ND | 1.18b |
bAmTroSPC (6) | 8 | 1 | 8 | 64 | 64 | 1 | 64 | 2.49 |
eAmSPC (7) | 2 | 0.5 | 4 | 4 | 1 | 4 | 4 | 1.01b |
eAmTroSPC (8) | 2 | 0.25 | 8 | 8 | 8 | 1 | 8 | 2.31 |
Amino TroSPC (11) | 16 | 2 | 8 | 64 | 64 | 1 | 32 | 0.64 |
AmTroSPC (13) | 64 | 8 | 8 | 64 | 64 | 1 | 128 | 2.71 |
aMIC assays were conducted using M. smegmatis strain MC2 155. Ribosome inhibition assays were conducted using ribosomes purified from M. smegmatis strain SZ380
bRibosomal IC50 for compounds 1, 5, and 7 were previously reported in ref. [20]
cLead SPA 1810 (Compound 39 from ref. [16]) was substituted for SPA 3. SPA 1810 possess an additional hydroxyl on the para position of the pyridine ring when compared to SPA 3
dRibosomal IC50 used for compound 3 was converted from µg/mL to µM from what was previously reported in ref. [16]