title: Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues.
abstract: A series of modafinil (1) analogues was 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 DAT, SERT and NET 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.
authors.affiliation: Medicinal Chemistry, National Institute on Drug Abuse - Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, MD 21224.
authors.forename: Jianjing
authors.initials: J
authors.lastname: Cao
authors.forename: Thomas E
authors.initials: TE
authors.lastname: Prisinzano
authors.forename: Oluyomi M
authors.initials: OM
authors.lastname: Okunola
authors.forename: Theresa
authors.initials: T
authors.lastname: Kopajtic
authors.forename: Matthew
authors.initials: M
authors.lastname: Shook
authors.forename: Jonathan L
authors.initials: JL
authors.lastname: Katz
authors.forename: Amy Hauck
authors.initials: AH
authors.lastname: Newman