Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375651 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A series of spiro-piperidine azetidinone were synthesized and evaluated as potential TRPV1 antagonists. An important issue of plasma stability was investigated and resolved. Further focused SAR study lead to the discovery of a potent antagonist with good oral pharmacokinetic profile in rat.
Graphical abstractA potent TRPV1 antagonist with good rat pharmacokinetic profile was discovered.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Dong Xiao, Anandan Palani, Robert Aslanian, Brian A. McKittrick, Andrew T. McPhail, Craig C. Correll, P. Tara Phelps, John C. Anthes, Diane Rindgen,