Cubyl amides: novel P2X 7 receptor antagonists

H Gunosewoyo, JL Guo, MR Bennett, MJ Coster…

文献索引：Gunosewoyo, Hendra; Guo, Jun Liu; Bennett, Maxwell R.; Coster, Mark J.; Kassiou, Michael Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 13 p. 3720 - 3723

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被引用次数: 22

摘要

Polycyclic amides 2 and 5–9 were successfully synthesised and their lipophilicity profiles were evaluated using reverse-phase HPLC. All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X7 selectivity.