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Cubyl amides: Novel P2X7 receptor antagonists

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Authors
Gunosewoyo, Hendra
Guo, J.
Bennett, M.
Coster, M.
Kassiou, M.
Date
2008
Type
Journal Article

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Gunosewoyo, Hendra and Guo, Jun Liu and Bennett, Maxwell R. and Coster, Mark J. and Kassiou, Michael. 2008. Cubyl amides: Novel P2X7 receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 18 (13): pp. 3720-3723.
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Bioorganic & Medicinal Chemistry Letters
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Abstract

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.