Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter

…, D Parrish, JR Deschamps, A Janowsky

Index: Froimowitz, Mark; Gu, Yonghong; Dakin, Les A.; Nagafuji, Pamela M.; Kelley, Charles J.; Parrish, Damon; Deschamps, Jeffrey R.; Janowsky, Aaron Journal of Medicinal Chemistry, 2007 , vol. 50, # 2 p. 219 - 232

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Citation Number: 25

Abstract

Methylphenidate analogues, in which the carbomethoxy has been replaced by an alkyl group and with different phenyl substituents, have been synthesized and tested in monoamine transporter assays. As predicted from a pharmacophore model, most of the RR/SS diastereomers showed high potency as dopamine reuptake inhibitors. Analogues with a 4-chlorophenyl group and an unbranched initial alkyl atom had consistently ...