Synthesis and biological evaluation of novel tetrahydroisoquinoline-C-aryl glucosides as SGLT2 inhibitors for the treatment of type 2 diabetes

• A series of novel tetrahydroisoquinoline-C-aryl glucosides were synthesized.
• They were evaluated for the inhibition of human SGLT2.
• The structure-activity relationship was discussed.
• Compound 13h exhibited equivalent in vitro inhibitory activity with dapagliflozin.

A series of novel tetrahydroisoquinoline-C-aryl glucosides has been synthesized and evaluated for the inhibition of human SGLT2. Compared with dapagliflozin, compound 13h exhibited equivalent in vitro inhibitory activity against SGLT2, which might become a promising candidate for the treatment of type 2 diabetes.

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