Discovery, synthesis and biological evaluation of novel glucokinase activators

被引：52

作者：

McKerrecher, D ^{[1
]}

Allen, JV ^{[1
]}

Bowker, SS ^{[1
]}

Boyd, S ^{[1
]}

Caulkett, PWR ^{[1
]}

Currie, GS ^{[1
]}

Davies, CD ^{[1
]}

Fenwick, ML ^{[1
]}

Gaskin, H ^{[1
]}

Grange, E ^{[1
]}

Hargreaves, RB ^{[1
]}

Hayter, BR ^{[1
]}

James, R ^{[1
]}

Johnson, KM ^{[1
]}

Johnstone, C ^{[1
]}

Jones, CD ^{[1
]}

Lackie, S ^{[1
]}

Rayner, JW ^{[1
]}

Walker, RP ^{[1
]}

机构：

[1] AstraZeneca UK, Cardiovasc & Gastrointestinal Area, Macclesfield SK10 4TG, Cheshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 08期

关键词：

diabetes; glucokinase; kinase activator;

D O I：

10.1016/j.bmcl.2005.01.087

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The identification, synthesis and SAR of a novel series of glucokinase activators is described. The interplay between lipophilicity, potency and physical properties is discussed, and compound 22 highlighted as having a suitable balance. In vivo pharmacokinetic and acute efficacy studies on this compound are also presented. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：2103 / 2106

页数：4

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