SARs at the monoamine transporters for a novel series of modafinil analogues

Jianjing Cao, Thomas E. Prisinzano, Oluyomi M. Okunola, Theresa Kopajtic, Matthew Shook, Jonathan L. Katz, Amy Hauck Newman

Research output: Contribution to journalArticlepeer-review

63 Scopus citations


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 locomotor-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.

Original languageEnglish
Pages (from-to)48-52
Number of pages5
JournalACS Medicinal Chemistry Letters
Issue number1
StatePublished - Jan 13 2011


  • SAR
  • modafinil analogues
  • monoamine transporters

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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