Calzaferri, Francesco published the artcileSynthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is purine preparation antiinflammatory activity mol docking pharmacokinetic study; xanthine preparation antiinflammatory activity mol docking pharmacokinetic study.
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.
Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.
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