| Literature DB >> 22078214 |
Stephanie Brumfield1, Julius J Matasi, Deen Tulshian, Michael Czarniecki, William Greenlee, Charles Garlisi, Hongchen Qiu, Kristine Devito, Shu-Cheng Chen, Yongliang Sun, Rosalia Bertorelli, Justin Ansell, William Geiss, Van-Duc Le, Gregory S Martin, Samuel A Vellekoop, James Haber, Melissa L Allard.
Abstract
Novel P2X(7) antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X(7) 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.Entities:
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Year: 2011 PMID： 22078214 DOI： 10.1016/j.bmcl.2011.10.037
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823