Tetrahydroquinoline sulfonamides as vasopressin 1b receptor anatgonists
| Autor: | Tony Priestley, Vaccaro Henry A, Andrew Stamford, Deborra E Mullins, Michael W. Miller, Tin-Yau Chan, Robert A. Hodgson, Scott Jack D, William J. Greenlee, Liwu Hong, Mario Guzzi, Sarah W. Li, Eric M. Parker, Geoffrey B. Varty, Jay Weinstein, Sue-Ing Lin, Mckittrick Brian A |
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| Rok vydání: | 2009 |
| Předmět: |
Receptors
Vasopressin Vasopressin Stereochemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Animals Humans Receptor Molecular Biology chemistry.chemical_classification Arginine vasopressin receptor 1B Sulfonamides Tetrahydroisoquinoline Antidiuretic Agents Organic Chemistry Antagonist Rats Sulfonamide chemistry Receptors Oxytocin Quinolines Molecular Medicine Piperidine Linker Antidiuretic Hormone Receptor Antagonists |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 19:6018-6022 |
| ISSN: | 0960-894X |
| Popis: | Vasopressin 1b (V1b) antagonists have been postulated as possible treatments for depression and anxiety. A novel series of potent and selective V1b antagonists has been identified starting from an in-house screen hit. The incorporation of a sulfonamide linker between a tetrahydroisoquinoline core and amino piperidine lead to the identification of a V1b antagonist with similar affinity for human and rat receptors. Further optimization of the right hand portion afforded potent V1b antagonists that possessed moderate to high selectivity over other receptors. |
| Databáze: | OpenAIRE |
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