Tetrahydroquinoline derivatives as opioid receptor antagonists.
| Autor: | Zhang C; Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. cunyu.a.zhang@gsk.com, Westaway SM, Speake JD, Bishop MJ, Goetz AS, Carballo LH, Hu M, Epperly AH |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jan 15; Vol. 21 (2), pp. 670-6. Date of Electronic Publication: 2010 Dec 08. |
| DOI: | 10.1016/j.bmcl.2010.12.010 |
| Abstrakt: | Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent antagonist 2v, endowed with 1.58nM (K(i)) functional activity against the μ opioid receptor. DMPK data suggest that novel tetrahydroquinoline analogs may be advantageous in peripheral applications. (Copyright © 2010 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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