| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376236 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
Clinical candidate AMG 517 (1) is a potent antagonist toward multiple modes of activation of TRPV1; however, it suffers from poor solubility. Analogs with various substituents at the R region of 3 were prepared to improve the solubility while maintaining the potent TRPV1 activity of 1. Compounds were identified that maintained potency, had good pharmacokinetic properties, and improved solubility relative to 1.
Graphical abstractAnalogs with various substituents at the R region of 3 were prepared to improve the solubility while maintaining the potent TRPV1 activity of clinical candidate AMG 517.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Markian M. Stec, Yunxin Bo, Partha P. Chakrabarti, Lillian Liao, Mqhele Ncube, Nuria Tamayo, Rami Tamir, Narender R. Gavva, James J.S. Treanor, Mark H. Norman,