Table 5.
The minimum inhibitory concentrations (MIC) against H37Rv Mycobacterium tuberculosis (Mtb) afforded by compounds 1, 151-d and 16b.
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Compound | R1 | R2 | cLogPa | H37Rv Mtb MIC (μM) | |||
GAST-Fe | 7H9/ADC | 7H9/glucose | 7H9/DPPC | ||||
1 |
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1.6 | > 100 | > 100 | > 100 | > 100 |
15a |
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3.6 | > 100 | > 100 | 100 | 9.4 |
15b |
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3.6 | > 100 | > 100 | > 100 | 12.5 |
15c |
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4.1 | > 100 | > 100 | 25 | 9.4 |
15d |
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4.1 | > 100 | > 100 | 9.4 | 6.3 |
16b |
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2.1 | > 100 | > 100 | 25 | 19 |
Calculated using ChemDraw (PerkinElmer, Waltham MA).