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Bioorg Med Chem Lett. 2012 Apr 15;22(8):2784-8. doi: 10.1016/j.bmcl.2012.02.087. Epub 2012 Mar 2.

Pyrazine-based Syk kinase inhibitors.

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  • 1Almirall-Barcelona Science Park Unit, Barcelona Science Park, 08028 Barcelona, Spain.


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.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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