Table 2. Inhibition of HadAB and HadBC Enzyme Complexes by 1,3-Diarylpyrazolyl-acylsulfonamides.

^aInhibition values of 1,3-diarylpyrazolyl-acylsulfonamides (50 μM) for HadAB (22 nM) and HadBC (130 nM) as measured with trans-2-C_16:1-CoA substrate (60 μM in the HadAB assay; 25 μM in the HadBC assay) using the spectrophotometric assay as described previously.¹⁴

^bMIC in Middlebrook 7H9/glucose/BSA/Tx). IC₅₀ values of the selected compounds for HadAB enzymatic complex were determined using GraFit (Version 5.0.13). Hill slopes were not constrained, ranging between 1–2.5. Compounds with solubility issues displayed greater variability in testing and resulted in higher Hill slopes upon IC₅₀ curve fitting.

^cIC₅₀ values are close to the enzyme concentration used in the assay (22 nM) and could be more potent than the calculated value. Data are means ± standard deviations of duplicate assays and represent two separate trials; nd, not determined.