Cpds R1 R4 R5 R6 R7 hlIC50a rlIC50a
1.1 H H H H H 12.5 NDc
2.1 Ph H H H H 2 20
2.2 4-pyridyl H H H H 5.5 20
2.3 iBu H H H H 2 12
2.4 Ph H Cl H H 2.5 20
2.5 iPr H Cl H H 2.4 20
2.6 cPrCH2- H Cl H H 2 2
2.7 Ph H H Cl H 0.6 2
2.8 iBu H H Cl H 0.25 2
2.9 cPrCH2- H H Cl H 0.5 2
2.10 neoPentyl H H Cl H 0.8 2
2.11 cPrCH2- H Cl Cl H 3 20
2.12 cPrCH2- H Cl F H 0.7 2
2.13 Et Me Me Cl H 0.6 17
2.14 Br(CH2)4- Me Me Cl H 0.6 6
2.15 cPrCH2- Me Me Cl H 0.5 6
2.16 cPrCH2- Me Me Me Me 0.2 3.5
ahlIC50, human liver FBPase, μM; brlIC50, rat liver FBPase, μM; cND, not determined
Table 2: N1-SAR of Desaminobenzimidazole Analogsa