molecules of the month

“compound 6g”

potent and orally available SGLT1/2 dual inh.

activity in diabetes glucose tolerance model

based on natural product phlorizin

Bioorg. Med. Chem. Lett., Jul. 5, 2020

Janssen R&D, Spring House, PA.

Structure of compound 6g
1 min read

“compound 6g” is an oral inhibitor of the sodium-glucose co-transporters (SGLTs) 1 and 2, intended for the treatment of hyperglycemia. SGLT2 selective inhibitors (gliflozins) are approved for treatment of type 2 diabetes, and an SGLT1/2 dual inhibitor is expected to result in greater glycemic control. Like other SGLT inhibitors, this molecule is based on a natural product scaffold, and the analogs don’t look super easy to make (I was surprised to see a BAST difluorination proceed in 74% yield on a highly substituted ketone prone to elimination).

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