Open AccessSARs at the Monoamine Transporters for a Novel Series of Modafinil Analogues
Author(s) -
Jianjing Cao,
Thomas E. Prisinzano,
Oluyomi M. Okunola,
Theresa Kopajtic,
Matthew Shook,
Jonathan L. Katz,
Amy Hauck Newman
Publication year - 2010
Publication title -
acs medicinal chemistry letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.065
H-Index - 66
ISSN - 1948-5875
DOI - 10.1021/ml1002025
Subject(s) - modafinil , monoamine neurotransmitter , covid-19 , computational biology , pharmacology , medicine , computer science , biology , disease , infectious disease (medical specialty) , receptor , serotonin
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.