SARs at the Monoamine Transporters for a Novel Series of Modafinil Analogues

[摘要]：A series of modafinil (1) analogues were synthesized wherein (1) para-halo substitutents were added to the aryl rings, (2) the sulfoxide function was removed, and (3) the primary amide group was replaced with secondary and tertiary amides and amines to investigate the effects of these chemical modifications on dopamine transporter, serotonin transporter, and norepinephrine transporter binding. In addition, the locomoter-stimulant effects in mice of (+/-) modafinil (1), its R- and S-enantiomers, and its para-chloro sulfinylacetamide analogue (5c) were compared to those of cocaine.

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