Cubyl amides: Novel P2X7 receptor antagonists
Author(s)
Gunosewoyo, Hendra
Guo, Jun Liu
Bennett, Maxwell R
Coster, Mark J
Kassiou, Michael
Griffith University Author(s)
Year published
2008
Metadata
Show full item recordAbstract
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.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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Journal Title
Bioorganic & Medicinal Chemistry Letters
Volume
18
Issue
13
Subject
Medicinal and biomolecular chemistry
Organic chemistry
Pharmacology and pharmaceutical sciences