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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors.
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1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors.

机译:1-萘基和4-吲哚基芳基烷基胺作为选择性单胺再摄取抑制剂。

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摘要

A series of enantiomerically pure 1-naphthyl and 4-indolyl arylalkylamines were prepared and evaluated for their binding affinities to the monoamine transporters. The two series of enantiomers displayed considerable differences in binding selectivity between the monoamine transporters, leading to the design of (S)-4-(3,4-dichlorophenyl)-4-(1H-indol-4-yl)-N-methylbutan-1-amine as a potent inhibitor for the dopamine and serotonin transporters.
机译:制备了一系列对映体纯的1-萘基和4-吲哚基芳基烷基胺,并评估了它们与单胺转运蛋白的结合亲和力。这两个系列的对映异构体在单胺转运蛋白之间的结合选择性上显示出显着差异,从而导致了(S)-4-(3,4-二氯苯基)-4-(1H-吲哚-4-基)-N-甲基丁烷的设计-1-胺是多巴胺和5-羟色胺转运蛋白的有效抑制剂。

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