Tetrahydro-4-quinolinamines identified as novel P2Y1 receptor antagonists

被引：25

作者：

Morales-Ramos, Angel I. ^{[1
]}

Mecom, John S. ^{[1
]}

Kiesow, Terry J. ^{[3
]}

Graybill, Todd L. ^{[3
]}

Brown, Gregory D. ^{[1
]}

Aiyar, Nambi V. ^{[2
]}

Davenport, Elizabeth A. ^{[4
]}

Kallal, Lorena A. ^{[4
]}

Knapp-Reed, Beth A. ^{[1
]}

Li, Peng ^{[1
]}

Londregan, Allyn T. ^{[1
]}

Morrow, Dwight M. ^{[4
]}

Senadhi, Shobha ^{[2
]}

Thalji, Reema K. ^{[1
]}

Zhao, Steve ^{[1
]}

Burns-Kurtis, Cynthia L. ^{[2
]}

Marino, Joseph P., Jr. ^{[1
]}

机构：

[1] GlaxoSmithKline, Metabol Pathways Ctr Excellence Drug Discovery, Dept Chem, King Of Prussia, PA 19406 USA

[2] GlaxoSmithKline, Metabol Pathways Ctr Excellence Drug Discovery, Dept Biol, King Of Prussia, PA 19406 USA

[3] GlaxoSmithKline, Mol Discovery Res, Dept Chem, Collegeville, PA 19426 USA

[4] GlaxoSmithKline, Mol Discovery Res, Dept Biochem, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 23期

关键词：

P2Y1; receptor; Antagonist; Platelet aggregation; Thrombosis; Tetrahydro-4-quinolinamine;

D O I：

10.1016/j.bmcl.2008.09.102

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

High-throughput screening of the GSK compound collection against the P2Y1 receptor identified a novel series of tetrahydro-4-quinolinamine antagonists. Optimal substitution around the piperidine group was pivotal for ensuring activity. An exemplar analog from this series was shown to inhibit platelet aggregation. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6222 / 6226

页数：5

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