Skip to main content
. 2020 Jun 12;63(13):7066–7080. doi: 10.1021/acs.jmedchem.0c00373

Table 1. m-Substituted Derivatives 1–10a.

graphic file with name jm0c00373_0010.jpg

code R % residual activity IC50 (μM)
1 3-CF3 42.0 ± 6.3  
2 3-Cl 101.6 ± 17.8  
3 3-OH 70.4 ± 21.8  
4 3-CH3 103.9 ± 4.8  
5 3-NH2 65.8 ± 9.6  
6 3-CONH2 20.9 ± 4.3 31.4 ± 10.3
7 3-CONHCH3 84.0 ± 9.1  
8 3-SO2NH2 28.6 ± 6.8  
9 3-COOH 27.2 ± 4.5  
10 3-CN 3.1 ± 1.0 6.3 ± 0.9
a

Inhibitory effect is expressed as percentage of residual enzymatic activity (at 100 μM ligand concentration) for all compounds and half-maximal inhibitory concentrations (IC50, μM) only for the most active candidates (residual activity ≤ 25%).