Tetrahydroquinoline sulfonamides as vasopressin 1b receptor anatgonists
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- 作者：Jack D. Scott ; Michael W. Miller ; Sarah W. Li ; Sue-Ing Lin ; Henry A. Vaccaro ; Liwu Hong ; Deborra E. Mullins ; Mario Guzzi ; Jay Weinstein ; Robert A. Hodgson ; Geoffrey B. Varty ; Andrew W. Stamford ; Tin-Y
- 关键词：Vasopressin ; V1b antagonist ; V1b receptor ; Anxiety ; Depression
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 November 2009
- 年：2009
- 卷：19
- 期：21
- 页码：6018-6022
- 全文大小：1035 K
文摘
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.