Glycosylated dihydrochalcones as potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitors

被引：58

作者：

Dudash, J ^{[1
]}

Zhang, XY ^{[1
]}

Zeck, RE ^{[1
]}

Johnson, SG ^{[1
]}

Cox, GG ^{[1
]}

Conway, BR ^{[1
]}

Rybczynski, PJ ^{[1
]}

Demarest, KT ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 20期

关键词：

D O I：

10.1016/j.bmcl.2004.07.082

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of glucose conjugates was synthesized and tested for inhibition of SGLT1 and SGLT2. The core structure was derived from compound la. Modification of the benzofuran moiety and 4-substituent of the phenyl ring in compound la improved selectivity at SGLT2. Select compounds were compared to la in metabolic stability and in vivo efficacy studies. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5121 / 5125

页数：5

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