Cpds |
R4 |
R5 |
R6 |
R7 |
hlIC50, µMa |
rlIC50, µMa |
2.8 |
H |
H |
Cl |
H |
0.25 |
2 |
3.1 |
H |
Cl |
H |
H |
0.6 |
20 |
3.2 |
H |
H |
F |
H |
1 |
2 |
3.3 |
H |
F |
H |
H |
0.8 |
2 |
3.4 |
H |
Br |
H |
H |
2.7 |
20 |
3.5 |
H |
H |
Br |
H |
0.7 |
2 |
3.6 |
HO |
H |
H |
H |
2.5 |
20 |
3.7 |
Me |
H |
H |
H |
1.75 |
20 |
3.8 |
H |
F |
F |
H |
0.45 |
2 |
3.9 |
H |
Cl |
Cl |
H |
2.2 |
2 |
3.10 |
H |
Cl |
F |
H |
0.95 |
2 |
3.11 |
H |
F |
NH2 |
Br |
1.2 |
5 |
3.12 |
H |
F |
F |
F |
1.55 |
10 |
3.13 |
F |
F |
F |
H |
0.5 |
6 |
3.14 |
Me |
Me |
Cl |
Br |
0.4 |
2.5 |
3.15 |
Br |
Cl |
Me |
Me |
0.75 |
2.7 |
3.16 |
Me |
Me |
Me |
Me |
0.25 |
2.25 |
aHLF, human liver FBPase; RLF, rat liver FBPase; glucose lowering was measured
after iv dosing of 10 mg/kg compounds. bND, not determined |