O'Brien-Brown, James
Jackson, Alexander
Reekie, Tristan A
Barron, Melissa L
Werry, Eryn L
Schiavini, Paolo
McDonnell, Michelle
Munoz, Lenka
Wilkinson, Shane
Noll, Benjamin
Wang, Shudong
Kassiou, Michael
2017-03-02
<p>Here we report adamantyl cyanoguanidine compounds based on hybrids of the adamantyl amide scaffold reported by AstraZeneca and cyanoguanidine scaffold reported by Abbott Laboratories. Compound 27 displayed five-fold greater inhibitory potency than the lead compound 2 in both pore-formation and interleukin-1β release assays, while 35-treated mice displayed an antidepressant phenotype in behavioral studies. This SAR study provides a proof of concept for hybrid compounds, which will help in the further development of P2X<sub>7</sub>R antagonists.</p>
https://doi.org/10.1016/j.ejmech.2017.02.060
oai:zenodo.org:400509
Zenodo
https://zenodo.org/communities/inmind
https://zenodo.org/communities/eu
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Eur J Med Chem., 130, 433-439, (2017-03-02)
ATP
Adamantane
Adamantyl
Alzheimer's
IL-1β
Inflammation
Neurodegenerative
P2X receptor
P2X(7)R antagonist
Discovery and pharmacological evaluation of a novel series of adamantyl cyanoguanidines as P2X7 receptor antagonists.
info:eu-repo/semantics/article