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.

DOI: 10.1016/j.bmcl.2008.05.062

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@article{Gunosewoyo2008CubylAN, title={Cubyl amides: novel P2X7 receptor antagonists.}, author={Hendra Gunosewoyo and Jun Liu Guo and Max R. Bennett and M. J. Coster and Michael Kassiou}, journal={Bioorganic & medicinal chemistry letters}, year={2008}, volume={18 13}, pages={3720-3} }