Synthesis and SAR development of novel P2X₇ receptor antagonists for the treatment of pain: Part 2

Novel P2X₇ antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X₇ receptor in human and rodent as well as efficacious in rodent pain models. Compound 15a was identified to have oral potency in several pain models in rodent similar to naproxen, gabap...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-12, Vol.21 (24), p.7287-7290
Hauptverfasser:	Brumfield, Stephanie, Matasi, Julius J, Tulshian, Deen, Czarniecki, Michael, Greenlee, William, Garlisi, Charles, Qiu, Hongchen, Devito, Kristine, Chen, Shu-Cheng, Sun, Yongliang, Bertorelli, Rosalia, Ansell, Justin, Geiss, William, Le, Van-Duc, Martin, Gregory S, Vellekoop, Samuel A, Haber, James, Allard, Melissa L
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics animal models Animals antagonists Biological and medical sciences Humans Medical sciences Neuropharmacology pain Pain - drug therapy Pharmacology. Drug treatments Purinergic P2X Receptor Antagonists - chemical synthesis Purinergic P2X Receptor Antagonists - chemistry Purinergic P2X Receptor Antagonists - therapeutic use Purines - chemical synthesis Purines - chemistry Purines - therapeutic use Rats Receptors, Purinergic P2X7 - chemistry Receptors, Purinergic P2X7 - metabolism rodents Structure-Activity Relationship structure-activity relationships
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Zusammenfassung:	Novel P2X₇ antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X₇ receptor in human and rodent as well as efficacious in rodent pain models. Compound 15a was identified to have oral potency in several pain models in rodent similar to naproxen, gabapentin and pregabalin. Structure–activity relationship (SAR) development and results of pain models are presented.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.10.037