Cpds R4 R5 R6 R7 IC50, µMa 1.1 H H H H 12.5 1.2 Me H H H 4 1.3 H Me H H 12 1.4 H F H H 3 1.5 H Cl H H 5 1.6 H Br H H 4.7 1.7 H CF3 H H 15 1.8 H F F H 1.8 1.9 H Cl Cl H 4.5 1.10 H F Cl H 3.5 1.11 H Me Me H 10 1.12 Cl H Cl H 5.2 1.13 Br H Br H 5.6 1.14 Br H F H 2.3 1.15 Me Me Me Me 0.9 aIC50, human liver FBPase; bND, not determined

Table 1: SAR of N1-H benzimidazole Phosphonic Acidsa