4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors

…, AS Vellekoop, AM Klos, PJ Crocker, C Hassler…

文献索引：Pechulis, Anthony D.; Beck, James P.; Curry, Matt A.; Wolf, Mark A.; Harms, Arthur E.; Xi, Ning; Opalka, Chet; Sweet, Mark P.; Yang, Zhicai; Vellekoop, A. Samuel; Klos, Andrew M.; Crocker, Peter J.; Hassler, Carla; Laws, Mia; Kitchen, Douglas B.; Smith, Mark A.; Olson, Richard E.; Liu, Shuang; Molino, Bruce F. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7219 - 7222

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被引用次数: 7

摘要

Novel 4-phenyl tetrahydroisoquinolines that inhibit both dopamine and norepinephrine transporters were designed and prepared. In this Letter, we describe the synthesis, in vitro activity and associated structure–activity relationships of this series. We also report the ex vivo NET occupancy of a representative compound, 41.