So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Calzaferri, Francesco; Narros-Fernandez, Paloma; de Pascual, Ricardo; de Diego, Antonio M. G.; Nicke, Annette; Egea, Javier; Garcia, Antonio G.; de los Rios, Cristobal researched the compound: 2,6-Dichloropurine( cas:5451-40-1 ).COA of Formula: C5H2Cl2N4.They published the article 《Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation》 about this compound( cas:5451-40-1 ) in Journal of Medicinal Chemistry. Keywords: purine preparation antiinflammatory activity mol docking pharmacokinetic study; xanthine preparation antiinflammatory activity mol docking pharmacokinetic study. We’ll tell you more about this compound (cas:5451-40-1).
In this work, novel blood-brain barrier (BBB)-permeable derivatives, e.g., I as potential P2X7 antagonists were designed and synthesized. They comprise purine or xanthine cores linked to an aryl group through different short spacers. Compounds were tested in YO-PRO-1 uptake assays and intracellular calcium dynamics in a human P2X7-expressing HEK293 cell line, two-electrode voltage-clamp in Xenopus laevis oocytes, and in interleukin 1β release assays in mouse peritoneal macrophages. BBB permeability was assessed by parallel artificial membrane permeability assays and P-glycoprotein ATPase activity. Dichloroarylpurinylethanones featured a certain P2X7 blockade, being compound (2-(6-chloro-9H-purin-9-yl)-1-(2,4-dichlorophenyl)ethan-1-one) (I), named ITH15004, the most potent, selective, and BBB-permeable antagonist. Compound I can be considered as a first non-nucleotide purine hit for future drug optimizations.
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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem