N-glucosides as human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitors

被引：22

作者：

Yamamoto, Yasuo ^{[1
]}

Kawanishi, Eiji ^{[1
]}

Koga, Yuichi ^{[1
]}

Sakamaki, Shigeki ^{[1
]}

Sakamoto, Toshiaki ^{[1
]}

Ueta, Kiichiro ^{[2
]}

Matsushita, Yasuaki ^{[2
]}

Kuriyama, Chiaki ^{[2
]}

Tsuda-Tsukimoto, Minoru ^{[3
]}

Nomura, Sumihiro ^{[1
]}

机构：

[1] Mitsubishi Tanabe Pharma Corp, Med Chem Res Labs, Toda, Saitama 3358505, Japan

[2] Mitsubishi Tanabe Pharma Corp, Pharmacol Res Labs, Toda, Saitama 3358505, Japan

[3] Mitsubishi Tanabe Pharma Corp, DMPK Res Labs, Toda, Saitama 3358505, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 20期

关键词：

SGLT2; Sodium-dependent glucose cotransporter; Diabetes; Glucoside; N-glucoside; NA+/GLUCOSE COTRANSPORTER; DIABETES-MELLITUS; SGLT2; INHIBITORS; MECHANISM; TYPE-2; REABSORPTION; DISCOVERY; POTENT; RING;

D O I：

10.1016/j.bmcl.2013.08.042

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibition of renal sodium-dependent glucose cotransporter 2 (SGLT2) increases urinary glucose excretion (UGE), and thus reduces blood glucose levels in hyperglycemia. A series of N-glucosides was synthesized for biological evaluation as human SGLT2 (hSGLT2) inhibitors. Among these compounds, N-glucoside 9d possessing an indole core structure showed good in vitro activity (IC50 = 7.1 nM against hSGLT2). Furthermore, 9d exhibited favorable in vivo potency with regard to UGE in rats based on good pharmacokinetic profiles. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：5641 / 5645

页数：5

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