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Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1 |
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| 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 |
| Institution: | a Merck Research Laboratories, 2015 Galloping Hill Road, MS 2800, Kenilworth, NJ 07033-0539, USA b Albany Molecular Research, Inc., 21 Corporate Circle, Albany, NY 12212-5098, USA |
| Abstract: | Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X7 receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and selective at the P2X7 receptor in both human and rodent. Compound (entry 31) exhibited oral efficacy in the rat MIA and CCI pain models. |
| Keywords: | P2X7 Purine derivatives Inflammatory pain Neuropathic pain |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |