Heteroaryl-O-glucosides as novel sodium glucose co-transporter 2 inhibitors. Part 1

Xiaoyan Zhang; Maud Urbanski; Mona Patel; Roxanne E Zeck; Geoffrey G Cox; Haiyan Bian; Bruce R Conway; Mary Pat Beavers; Philip J Rybczynski; Keith T Demarest

doi:10.1016/j.bmcl.2005.08.067

Heteroaryl-O-glucosides as novel sodium glucose co-transporter 2 inhibitors. Part 1

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5202-6. doi: 10.1016/j.bmcl.2005.08.067. Epub 2005 Sep 28.

Authors

Xiaoyan Zhang¹, Maud Urbanski, Mona Patel, Roxanne E Zeck, Geoffrey G Cox, Haiyan Bian, Bruce R Conway, Mary Pat Beavers, Philip J Rybczynski, Keith T Demarest

Affiliation

¹ Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 1000 Rt. 202, PO Box 300, Raritan, NJ 08869, USA. [email protected]

PMID: 16198559
DOI: 10.1016/j.bmcl.2005.08.067

Abstract

A series of benzo-fused heteroaryl-O-glucosides was synthesized and evaluated in SGLT1 and 2 cell-based functional assays. Indole-O-glucoside 10a and benzimidazole-O-glucoside 18 exhibited potent in vitro SGLT2 inhibitory activity.

MeSH terms

Glucosides / chemical synthesis
Glucosides / chemistry*
Glucosides / pharmacology*
Humans
Molecular Structure
Sodium-Glucose Transporter 2 Inhibitors*

Substances

Glucosides
Sodium-Glucose Transporter 2 Inhibitors