Table 1. In Vitro Activity of Azide 3, Amine 6, Desazido BTZ, 8, and Click Chemistry Products 9–11 and Controls against H37Rv Strain of Mtb (in 7H12 and GAS Media)a.
| compd | MABA:MIC 7H12 (μM) | MABA:MIC GAS(μM) | MIC NTB1 |
|---|---|---|---|
| 3 | 0.47 | 0.46 | 0.5 |
| 6b | >10 (12%) | >10 (10%) | |
| 8 | >100 | 8.68 | |
| 9 | 0.87 | 0.95 | |
| 10c | 9.90 | 9.27 | |
| 11d | 0.93 | >1 | |
| 1 (BTZ043) | <0.004 | < 0.004 | |
| rifampin | 0.05 | 0.04 |
a
MABA, microplate alamar blue assay; GAS, glycerol-alanine-salts medium; 7H12, 7H9 medium plus casitone, palmitic acid, albumin, and catalase.
b
87% and 0% inhibition was observed at a concentration of >1 μM for 7H12 and GAS media, respectively.
c
0% inhibition was observed at >1 μM concentration for both 7H12 and GAS media.
d
34% inhibition was observed at >1 μM concentration for GAS media. NTB1, Mtb strain with Cys387Ser mutation.