Article ID Journal Published Year Pages File Type
1377420 Bioorganic & Medicinal Chemistry Letters 2007 5 Pages PDF
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
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