Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity

被引：43

作者：

Guertin, KR ^{[1
]}

Setti, L ^{[1
]}

Qi, L ^{[1
]}

Dunsdon, RM ^{[1
]}

Dymock, BW ^{[1
]}

Jones, PS ^{[1
]}

Overton, H ^{[1
]}

Taylor, M ^{[1
]}

Williams, G ^{[1
]}

Sergi, JA ^{[1
]}

Wang, K ^{[1
]}

Peng, Y ^{[1
]}

Renzetti, M ^{[1
]}

Boyce, R ^{[1
]}

Falcioni, F ^{[1
]}

Garippa, R ^{[1
]}

Olivier, AR ^{[1
]}

机构：

[1] Hoffmann La Roche Inc, Roche Res Ctr, Nutley, NJ 07110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(03)00623-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents have been identified. These compounds show non-selective inhibitory properties against a panel of protein tyrosine phosphatases including PTP1B. Compounds 12 and 13 display oral glucose lowering effects in ob/ob mice. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：2895 / 2898

页数：4

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