Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators

被引：48

作者：

Nishimura, Teruyuki ^{[1
]}

Iino, Tomoharu ^{[1
]}

Mitsuya, Morihiro ^{[1
]}

Bamba, Makoto ^{[1
]}

Watanabe, Hitomi ^{[1
]}

Tsukahara, Daisuke ^{[1
]}

Kamata, Kenji ^{[1
]}

Sasaki, Kaori ^{[1
]}

Ohyama, Sumika ^{[1
]}

Hosaka, Hideka ^{[1
]}

Futamura, Mayumi ^{[1
]}

Nagata, Yasufumi ^{[1
]}

Eiki, Jun-ichi ^{[1
]}

机构：

[1] Banyu Pharmaceut Co Ltd, Banyu Tsukuba Res Inst, Tsukuba, Ibaraki 3002611, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 05期

关键词：

Glucokinase; Glucokinase activator; Diabetes; GLUCOSE; DISCOVERY; EFFICACY;

D O I：

10.1016/j.bmcl.2009.01.053

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The identification and structure-activity-relationships (SARs) of novel 2-amino benzamide glucokinase activators are described. Compounds in this series were developed to be potent GK activators, and their binding mode to the GK protein was determined by crystal structure analysis. In vivo pharmacokinetic and acute in vivo efficacy studies of compound 18 are also described. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1357 / 1360

页数：4

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