Cubyl amides: Novel P2X7 receptor antagonists

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Author(s)
Gunosewoyo, Hendra
Guo, Jun Liu
Bennett, Maxwell R
Coster, Mark J
Kassiou, Michael
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Dr. D L Boger, L Ghosez, M. Shibasaki

Date
2008
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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.

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Bioorganic & Medicinal Chemistry Letters

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18

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13

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Medicinal and biomolecular chemistry

Organic chemistry

Pharmacology and pharmaceutical sciences

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