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Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2010-10-28 , DOI: 10.1016/j.bmcl.2010.10.086
Liming Shao , Jianguo Ma , Fengjiang Wang , Scott C. Malcolm , Michael C. Hewitt , Una C. Campbell , Nancy A. Spicer , Larry W. Hardy , Rudy Schreiber , Kerry L. Spear , Mark A. Varney

The present work describes a series of novel tetrahydroquinoline amines that potently inhibit the in vitro reuptake of serotonin and dopamine (dual reuptake inhibitors). The compounds are structurally related to a series we disclosed previously, but are improved with respect to cytochrome P-450 enzyme (CYP) and potassium ion channel Kv11.1 (hERG) inhibition and synthetic accessibility. The detailed synthesis and in vitro activity and ADME profile of the compounds is described, which represent a previously undisclosed dual reuptake inhibitor chemotype.

中文翻译:

发现 1-(3,4-二氯苯基)-N,N-二甲基-1,2,3,4-四氢喹啉-4-胺,一种血清素和多巴胺再摄取双重抑制剂

目前的工作描述了一系列新型四氢喹啉胺,它们可有效抑制体外血清素和多巴胺(双重再摄取抑制剂)的再摄取。这些化合物在结构上与我们之前公开的一系列化合物相关,但在细胞色素 P-450 酶 (CYP) 和钾离子通道 Kv11.1 (hERG) 抑制和合成可及性方面有所改进。描述了这些化合物的详细合成、体外活性和 ADME 概况,它们代表了先前未公开的双重再摄取抑制剂化学类型。
更新日期:2010-10-28
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