On April 20, 2016, Ziff, Jeannie; Rudolph, Dale A.; Stenne, Brice; Koudriakova, Tatiana; Lord, Brian; Bonaventure, Pascal; Lovenberg, Timothy W.; Carruthers, Nicholas I.; Bhattacharya, Anindya; Letavic, Michael A.; Shireman, Brock T. published an article.COA of Formula: C28H32N4O2S The title of the article was Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 Antagonists. And the article contained the following:
We describe the synthesis of a novel class of brain penetrating P2X7 antagonists with high potency at both the rat and human P2X7 receptors. Disclosed herein are druglike mols. with demonstrated target engagement of the rat P2X7 receptors after an oral dose. Specifically, compound 20 occupied the P2X7 receptors >80% over the 6 h time course as measured by an ex vivo radioligand binding experiment In a dose-response assay, this mol. has a plasma EC50 of 8 ng/mL. Overall, 20 has suitable druglike properties and pharmacokinetics in rat and dog. This mol. and others disclosed herein will serve as addnl. tools to elucidate the role of the P2X7 receptor in neuropsychiatric disorders. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).COA of Formula: C28H32N4O2S
The Article related to dihydropyrido pyrimidinyl methanone derivative preparation p2x7 antagonist, 5,6-dihydropyrido[3,4-d]pyrimidin-7(8h)-yl) methanones, cns, il-1β, p2x7, depression, neuroinflammation and other aspects.COA of Formula: C28H32N4O2S
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Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics