| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370134 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Stephanie Brumfield, 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,