Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377420 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
It has been hypothesized that peripherally restricted NMDA receptor antagonists may be effective analgesics for osteoarthritis pain. A class of novel quinoxalinedione atropisomers, first discovered for an NMDA receptor antagonist program for the treatment of stroke, was evaluated and further optimized with the goal of finding peripherally restricted NMDA receptor antagonists.
Graphical abstractA series of quinoxalinedione sulfonamides with potent NMDA receptor antagonist activity are discussed as potential pain therapeutics. The antagonists were optimized for oral bioavailability and decreased capacity to cross the blood–brain barrier.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christopher Deur, Arun K. Agrawal, Heidi Baum, John Booth, Susan Bove, Joan Brieland, Amy Bunker, Cleo Connolly, Joseph Cornicelli, JoAnn Dumin, Barry Finzel, Xinmin Gan, Sheila Guppy, Gregg Kamilar, Kenneth Kilgore, Pil Lee, Cho-Ming Loi, Zhen Lou,