Cubyl amides: Novel P2X7 receptor antagonists

Gunosewoyo, Hendra; Guo, Jun Liu; Bennett, Maxwell R; Coster, Mark J; Kassiou, Michael

doi:10.1016/j.bmcl.2008.05.062

Author(s)

Gunosewoyo, Hendra

Guo, Jun Liu

Bennett, Maxwell R

Coster, Mark J

Kassiou, Michael

Griffith University Author(s)

Coster, Mark J.

Year published

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.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

Issue

DOI

https://doi.org/10.1016/j.bmcl.2008.05.062

Subject

Medicinal and biomolecular chemistry

Organic chemistry

Pharmacology and pharmaceutical sciences

Publication URI

http://hdl.handle.net/10072/23680

Collection

Journal articles