| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365399 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating α-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and good bioavailability in the rat and dog. In addition, these functionally active compounds show high passive permeability and low susceptibility to phosphoglycoprotein mediated efflux, predictive of good CNS exposure.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Michael R. Wood, Kathy M. Schirripa, June J. Kim, Scott D. Kuduk, Ronald K. Chang, Christina N. Di Marco, Robert M. DiPardo, Bang-Lin Wan, Kathy L. Murphy, Richard W. Ransom, Raymond S.L. Chang, Marie A. Holahan, Jacquelynn J. Cook, Wei Lemaire,