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. 2021 Feb 2;7(2):435–444. doi: 10.1021/acsinfecdis.0c00788

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

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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
a

IC50 values were determined by the DTNB assay with 50 nM Lpd.