Pyrazine-based Syk kinase inhibitors

被引：18

作者：

Forns, Pilar

Esteve, Cristina ^{[1
]}

Taboada, Lorena ^{[1
]}

Antonio Alonso, Juan ^{[1
]}

Orellana, Adelina ^{[1
]}

Maldonado, Monica ^{[1
]}

Carreno, Cristina ^{[1
]}

Ramis, Isabel ^{[1
]}

Lopez, Manel ^{[1
]}

Miralpeix, Montserrat ^{[1
]}

Vidal, Bernat ^{[1
]}

机构：

[1] Almirall, Almirall Res Ctr, E-08980 Barcelona, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 08期

关键词：

Syk; 2-Aminopyrazine; LAD2; TYROSINE KINASE; BIOLOGY;

D O I：

10.1016/j.bmcl.2012.02.087

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay. (C) 2012 Elsevier Ltd. All rights reserved.

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收藏

页码：2784 / 2788

页数：5

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