Pyrazine-based Syk kinase inhibitors

…, A Orellana, M Maldonado, C Carreño, I Ramis…

文献索引：Forns, Pilar; Esteve, Cristina; Taboada, Lorena; Alonso, Juan Antonio; Orellana, Adelina; Maldonado, Monica; Carreno, Cristina; Ramis, Isabel; Lopez, Manel; Miralpeix, Montserrat; Vidal, Bernat Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 8 p. 2784 - 2788

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被引用次数: 14

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.