Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors
S Sakamuri, IJ Enyedy, AP Kozikowski…
Index: Sakamuri, Sukumar; Enyedy, Istvan J; Kozikowski, Alan P; Zaman, Wahiduz A; Johnson, Kenneth M; Wang, Shaomeng Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 4 p. 495 - 500
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Citation Number: 25
Abstract
Pharmacophore-based discovery, synthesis, and structure–activity relationship (SAR) of a series of 4-phenyl-1-arylalkyl piperidines are disclosed. These compounds have been evaluated for their ability to inhibit reuptake of dopamine (DA) into striatal nerve endings (synaptosomes). The lead compound 5 and the most potent analogue 43 were found to have significant functional antagonism.
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