Chromenones as potent bradykinin B1 antagonists.
| Autor: | Bryan MC; Department of Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA., Biswas K, Peterkin TA, Rzasa RM, Arik L, Lehto SG, Sun H, Hsieh FY, Xu C, Fremeau RT, Allen JR |
|---|---|
| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Jan 01; Vol. 22 (1), pp. 619-22. Date of Electronic Publication: 2011 Oct 28. |
| DOI: | 10.1016/j.bmcl.2011.10.068 |
| Abstrakt: | A series of fused 6,6-bicyclic chromenones was investigated for activity against the bradykinin B1 receptor. SAR studies based on a pharmacophore model revealed compounds with high affinity for both human and rabbit B1. These compounds demonstrated favorable pharmacokinetic properties and 5-chlorochromenone 15 was efficacious in a carrageenan-induced mechanical hyperalgesia model for chronic pain. (Copyright © 2011 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
| Externí odkaz: |
|
Full Text from ScienceDirect