Table 3

Cpds	R⁴	R⁵	R⁶	R⁷	hlIC₅₀, µM^a	rlIC₅₀, µM^a
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

Table 3: Benzimidazole SAR of compound 2.3 Analogsa.