Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators

被引：38

作者：

Iino, Tomoharu ^{[1
]}

Sasaki, Yasuhiro ^{[1
]}

Bamba, Makoto ^{[1
]}

Mitsuya, Morihiro ^{[1
]}

Ohno, Akio ^{[1
]}

Kamata, Kenji ^{[1
]}

Hosaka, Hideka ^{[1
]}

Maruki, Hiroko ^{[1
]}

Futamura, Mayumi ^{[1
]}

Yoshimoto, Riki ^{[1
]}

Ohyama, Sumika ^{[1
]}

Sasaki, Kaori ^{[1
]}

Chiba, Masato ^{[1
]}

Ohtake, Norikazu ^{[1
]}

Nagata, Yasufumi ^{[1
]}

Eiki, Jun-ichi ^{[1
]}

Nishimura, Teruyuki ^{[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 / 19期

关键词：

Glucokinase; Glucokinase activator; Glucose lowering efficacy; Log D; Aqueous solubility; 4,6-Disubstituted quinazoline; POTENT; SOLUBILITY; BENZAMIDES; EFFICACY;

D O I：

10.1016/j.bmcl.2009.08.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe design, syntheses and structure-activity relationships of a novel class of 4,6-disubstituted quinazoline glucokinase activators. Prototype quinazoline leads (4 and 5) were designed based on the X-ray analyses of the previous 2-aminobenzamide lead classes. Modifications of the quinazoline leads led to the identification of a potent GK activator (21d). (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5531 / 5538

页数：8

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