Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT 2C receptor
| Autor: | Minh Le, Albert S. Ren, Andrew J. Grottick, Graeme Semple, Kevin Whelan, Kelli Chase, Carleton R. Sage, Bilal Al Doori, Jenny Dong, Michelle Kasem, Chunrui Wu, Konrad Feichtinger, Jing Wei, Thomas O. Schrader, Huong T. Dang, Joel Gatlin |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Stereochemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Lorcaserin 03 medical and health sciences 0302 clinical medicine Drug Discovery medicine Potency Receptor Molecular Biology 5-HT receptor chemistry.chemical_classification Chemistry Organic Chemistry Combinatorial chemistry In vitro 5-HT2C receptor 030104 developmental biology Molecular Medicine Selectivity 030217 neurology & neurosurgery medicine.drug Tricyclic |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 26:5877-5882 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2016.11.016 |
| Popis: | The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT2C receptor agonists are reported. An early lead containing a highly unique 6,6,7-ring system was optimized for both in vitro potency and selectivity at the related 5-HT2B receptor. Orally bioactive, potent, and selective 6,6,6-tricyclic 5-HT2C agonists were identified. |
| Databáze: | OpenAIRE |
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