Table 2. SAR Analysis, Antibacterial Activity, and ADME Profiling of Sulfonamide Analogsa.

| no. | R | Lpd IC50 (μM) | Mtb MIC90 (μM) | Sol (μg/mL, pH 6.8) | hLM (μL/min/mg) | log D |
|---|---|---|---|---|---|---|
| 2 | a | 0.104 | >100 | 4.6 | 115 | 1.85 |
| 3 | b | 1.70 | >100 | 0.15 | 113 | 1.94 |
| 4 | c | 0.11 | >100 | >110 | 2 | 1.69 |
| 5 | d | 0.128 | >100 | >120 | 15 | 2.12 |
| 6 | e | 0.056 | >100 | 20 | 18 | 2.12 |
| 7 | f | 0.196 | >100 | >100 | –14 | 1.37 |
| 8 | g | 0.331 | >100 | >97 | 6 | 1.32 |
| 9 | h | 2.75 | >100 | >95 | –18 | 0.4 |
| 10 | i | 0.165 | >100 | >97 | 13 | 0.45 |
| 11 | a | 0.035 | 25 | 18 | >768 | 2.26 |
| 12 | e | 0.029 | 12 | 23 | 195 | 2.55 |
| 13 | i | 0.045 | 3.1 | >110 | –11 | 0.83 |
IC50 values were determined by the DTNB assay with 50 nM Lpd.