Pyrazine-based Syk kinase inhibitors

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

Index: 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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Citation Number: 14

Abstract

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.