Synthesis and SAR development of novel P2X 7 receptor antagonists for the treatment of pain: Part 1

JJ Matasi, S Brumfield, D Tulshian, M Czarnecki…

Index: Matasi, Julius J.; Brumfield, Stephanie; Tulshian, Deen; Czarnecki, Michael; Greenlee, William; Garlisi, Charles G.; Qiu, Hongchen; Devito, Kristine; Chen, Shu-Cheng; Sun, Youngliang; Bertorelli, Rosalia; Geiss, William; Le, Van-Duc; Martin, Gregory S.; Vellekoop, Samuel A.; Haber, James; Allard, Melissa L. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 12 p. 3805 - 3808

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Citation Number: 12

Abstract

Abstract Structure–activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X 7 receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and selective at the P2X 7 receptor in both human and rodent. Compound (entry 31) exhibited oral efficacy in the rat MIA and CCI pain models.

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