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. 2011 Mar 11;2(5):402–406. doi: 10.1021/ml200045s

Table 1. SAR and PK Properties of GSNOR Inhibitors.

compd R1 R2 R3 GSNOR IC50 (nM) % F CL (mL/min/kg)
5a H H H 570 86.5 8.9
5b H H Me 360 46.8 11.8
5c OMe H H 460    
5d OMe H F 240    
5e OMe H Cl 190    
14 OMe H CF3 450    
5f OMe H Me 210 16.2 35.4
13a F H Me 500    
13b Cl H Me 120 20.7 16.0
13c Br H Me 160 18.0 21.4
5g CN H Me 563 16.3 25.5
5h OH H Me 160    
13d CF3 H Me 3990    
15 CONH2 H Me 3920    
N6022 1H-imidazol-1-yl H Me 20 4.4 37.8
16 Cl MeO Me 56 22.4 20.2
13e MeO Cl Me 200    
17 Br MeO Me 96 21.8 22.4
5j Cl OH Me 55 2.72 33.4
13f Cl CONH2 Me 160    
18 Cl EtO Me 170    
19 Cl PrO Me 110    
20 Cl NMe2 Me 350    
21 Cl NHCHO Me 580    
13g Cl Cl Me 160    
13h Cl F Me 120    
13i Cl CF3 Me 330