化学
脚手架
药理学
酰胺
铅化合物
效力
受体
立体化学
组合化学
体外
生物化学
医学
生物医学工程
作者
James O’Brien-Brown,Alexander Jackson,Nils Trapp,Melissa L. Barron,Eryn L. Werry,Paolo Schiavini,Michelle N. McDonnell,Lenka Munoz,Shane M. Wilkinson,Benjamin Noll,Shudong Wang,Michael Kassiou
标识
DOI:10.1016/j.ejmech.2017.02.060
摘要
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 P2X7R antagonists.
科研通智能强力驱动
Strongly Powered by AbleSci AI