Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists
| Autor: | Beverly P. Holskin, Karla Kopec, Joanne R. Mathiasen, Amy DiCamillo, Babu G. Sundar, Thomas J. Connors, Emir Duzic, Edward R. Bacon, Gerard C. Rosse, Chrysanthe Spais, Thomas R. Bailey, Beth Ann McKenna, Rebecca A. Brown, Jie Qian, Derek Dunn, Mark J. Huffman, Joseph M. Salvino, Huang Zeqi, Lisa D. Aimone, Hervé Schaffhauser, Deborah Galinis, Thelma S. Angeles, Lily D. Lu, George C. Morton |
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| Rok vydání: | 2012 |
| Předmět: |
biology
Organic Chemistry Clinical Biochemistry hERG Pharmaceutical Science Pharmacology Biochemistry Social recognition chemistry.chemical_compound chemistry Drug Discovery biology.protein 5-HT6 receptor Molecular Medicine Structure–activity relationship Serotonin Antagonists Penetrant (biochemical) Receptor Molecular Biology 5-HT receptor |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 22:120-123 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.11.050 |
| Popis: | 7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT(6) receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, brain penetrant antagonists with reduced hERG liability. An advanced analog tested in rat social recognition model showed significant activity suggesting potential utility in the enhancement of short-term memory. |
| Databáze: | OpenAIRE |
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