TABLE 1.
NSC compound no. | MIC (μg/ml)
|
Concn (μg/ml) tested with macrophages | Efficacy in macrophage model | |
---|---|---|---|---|
L. tarentolae | L. major | |||
377 | 0.015 | 0.25 | 0.03 | − |
4972 | 0.2 | 1 | 0.4 | − |
687330 | 20 | 5 | 2 | − |
108944 | 11 | 5.5 | 1.1 | − |
163443 | 15.5 | 8 | 1.6 | − |
635975 | 8 | 8 | 0.8 | − |
165883 | 0.5 | 9 | 0.9 | − |
46613 | 9.5 | 9.5 | 1 | − |
63984 | 10 | 10 | 1 | − |
634650 | 10 | 10 | 1 | − |
112789 | 11 | 10.5 | 1.1 | − |
150169 | 10.5 | 10.5 | 1.1 | − |
97703 | 11 | 11 | 1.1 | − |
687667 | 11 | 11 | 1.1 | − |
168466 | 2.5 | 11 | 1.1 | − |
150554 | 1.5 | 11.5 | 1.2 | − |
50155 | 3 | 11.5 | 1.2 | − |
58319 | 3 | 12 | 1.2 | − |
128305 | 12.5 | 12.5 | 1.3 | − |
648422 | 109 | 13 | 1.3 | − |
89110 | 3 | 13 | 6.5 | − |
369294 | 109 | 13.5 | 11 | − |
647613 | 14 | 14 | 1.4 | − |
57584 | 14 | 14 | 1.4 | − |
281245 | 15.5 | 15.5 | 1.6 | − |
62791 | 16 | 16 | 1.6 | − |
176555 | 132 | 16.5 | 13 | − |
99504 | 67 | 17 | 13 | − |
273829 | 17.5 | 17.5 | 1.8 | − |
63984 | 10 | 20 | 1 | − |
13726 | 6.5 | 27 | 13.6 | − |
118770 | 7 | 27 | 11 | − |
7962 | 1.5 | 28.5 | 3.5 | − |
83633 | 29 | 29 | 12 | + |
62791 | 16 | 31.5 | 1.6 | − |
32673 | 0.13 | 33 | 0.3 | − |
56939 | 0.3 | 34.5 | 0.5 | − |
69298 | 5 | 38 | 9.5 | − |
281668 | 37 | 74 | 7.4 | − |
1199 | 11 | 90 | 9 | − |
351520 | 6.5 | 106 | 10.6 | + |
13512 | 29.5 | 117 | 12 | + |
35761 | 70.5 | 140 | 7 | − |
128164 | 38 | 152 | 15 | − |
73109 | 156 | 156 | 15.6 | − |
Pentostam | Not tested | 250 | 75 | + |
The MIC values against L. tarentolae and L. major were determined as described in Materials and Methods. In addition, the efficacy of each compound tested at the indicated concentrations in the macrophage infection model was determined as described in the Materials and Methods (+, activity; −, no activity).