Benzofuran-substituted urea derivatives as novel P2Y1 receptor antagonists

被引:29
作者
Thalji, Reema K. [1 ]
Aiyar, Nambi [2 ]
Davenport, Elizabeth A. [3 ]
Erhardt, Joseph A. [4 ]
Kallal, Lorena A. [3 ]
Morrow, Dwight M. [5 ]
Senadhi, Shobha [2 ]
Burns-Kurtis, Cynthia L. [2 ]
Marino, Joseph P., Jr. [6 ]
机构
[1] GlaxoSmithKline Inc, Dept Chem, Infect Dis Ctr Excellence Drug Discovery, Collegeville, PA 19426 USA
[2] GlaxoSmithKline Inc, Dept Biol, Metab Pathways Ctr Excellence Drug Discovery, King Of Prussia, PA 19406 USA
[3] GlaxoSmithKline Inc, Dept Biol Reagents & Assay Dev, Collegeville, PA 19426 USA
[4] GlaxoSmithKline Inc, Canc Res, Collegeville, PA 19426 USA
[5] GlaxoSmithKline Inc, Stem Cell Discovery Performance Unit, Collegeville, PA 19426 USA
[6] GlaxoSmithKline Inc, Metab Pathways Ctr Excellence Drug Discovery, Dept Chem, King Of Prussia, PA 19406 USA
关键词
P2Y(1); Purinergic; Thrombosis; Antiplatelet; Urea; P2; RECEPTORS; AGONISTS; ATP;
D O I
10.1016/j.bmcl.2010.05.072
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Benzofuran-substituted urea analogs have been identified as novel P2Y(1) receptor antagonists. Structure activity relationship studies around the urea and the benzofuran moieties resulted in compounds having improved potency. Several analogs were shown to inhibit ADP-mediated platelet activation. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4104 / 4107
页数:4
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