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

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

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) exhibi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters Vol. 21; no. 12; pp. 3805 - 3808
Main Authors: 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.
Format: Journal Article
Language:English
Published: Elsevier Ltd 15-06-2011
Subjects:
Inflammatory pain
Neuropathic pain
P2X 7
Purine derivatives
P2X 7
Purine derivatives
Inflammatory pain
Neuropathic pain
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.04.034