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Introduction of pyridine-containing prodrug moieties into tricyclic-based FBPase inhibitors led to the discovery of prodrug
20, which showed reduced CYP3A4 inhibitory potency compared to diamide prodrug
4.
For the purpose of reducing the strong CYP3A4 inhibitory potency of diamide prodrug
4, cyclic prodrugs of tricyclic-based FBPase inhibitors were synthesized. Extensive SAR studies led to the discovery of pyridine-containing cyclic prodrug
20, which strongly inhibited glucose production in monkey hepatocytes and also showed weak CYP3A4 inhibitory potency.