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Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.

Abstract：

:Inhibition of sodium-dependent glucose transporter 2 (SGLT2), the transporter that is responsible for renal re-uptake of glucose, leads to glucosuria in animals. SGLT-mediated glucosuria provides a mechanism to shed excess plasma glucose to ameliorate diabetes-related hyperglycemia and associated complications. The current study demonstrates that the proper relationship of a 4'-substituted benzyl group to a beta-1C-phenylglucoside is important for potent and selective SGLT2 inhibition. The lead C-arylglucoside (7a) demonstrates superior metabolic stability to its O-arylglucoside counterpart (4) and it promotes glucosuria when administered in vivo.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ellsworth BA,Meng W,Patel M,Girotra RN,Wu G,Sher PM,Hagan DL,Obermeier MT,Humphreys WG,Robertson JG,Wang A,Han S,Waldron TL,Morgan NN,Whaley JM,Washburn WN

doi

10.1016/j.bmcl.2008.07.109

subject

Has Abstract

pub_date

2008-09-01 00:00:00

pages

4770-3

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00893-7

journal_volume

18

pub_type

杂志文章

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