Cubyl amides: Novel P2X7 receptor antagonists

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.

Cubyl amides were successfully synthesised. All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells.Figure optionsDownload as PowerPoint slide