Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression

JR Cashman, T Voelker, R Johnson…

文献索引：Cashman, John R.; Voelker, Troy; Johnson, Robert; Janowsky, Aaron Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 1 p. 337 - 343

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被引用次数: 20

摘要

Multi-target compounds where more than one functional activity is incorporated into the same molecule may have advantages in treating disease states. Selective serotonin re- uptake inhibitors (SSRIs) a (ie,(R)-and (S)-norfluoxetine) were chemically linked to a PDE4 inhibitor via a five carbon bridge. The new dual PDE4 inhibitor/SSRIs (ie,(R)-8 and (S)-8) showed moderately potent but highly selective serotonin re-uptake inhibition (IC50 values ...