Article ID Journal Published Year Pages File Type
1375651 Bioorganic & Medicinal Chemistry Letters 2009 5 Pages PDF
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
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