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Pyrazine-based Syk kinase inhibitors |
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| Authors: | Forns Pilar Esteve Cristina Taboada Lorena Alonso Juan Antonio Orellana Adelina Maldonado Mónica Carreño Cristina Ramis Isabel López Manel Miralpeix Montserrat Vidal Bernat |
| Institution: | Almirall-Barcelona Science Park Unit, Barcelona Science Park, 08028 Barcelona, Spain. |
| 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. |
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