| Autor: |
Takeuchi K; Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA. ktak@Lilly.com, Holloway WG, McKinzie JH, Suter TM, Statnick MA, Surface PL, Emmerson PJ, Thomas EM, Siegel MG, Matt JE, Wolfe CN, Mitch CH |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Oct 01; Vol. 17 (19), pp. 5349-52. Date of Electronic Publication: 2007 Aug 11. |
| DOI: |
10.1016/j.bmcl.2007.08.008 |
| Abstrakt: |
A structurally unique and new class of opioid receptor antagonists (OpRAs) that bear no structural resemblance with morphine or endogenous opioid peptides has been discovered. A series of carboxamido-biaryl ethers were identified as potent receptor antagonists against mu, kappa and delta opioid receptors. The structure-activity relationship indicated para-substituted aryloxyaryl primary carboxamide bearing an amine tether on the distal phenyl ring was optimal for potent in vitro functional antagonism against three opioid receptor subtypes. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
Full Text from ScienceDirect