title: Convenient synthesis and biological evaluation of modafinil derivatives: benzhydrylsulfanyl and benzhydrylsulfinyl [1,2,3]triazol-4-yl-methyl esters.
abstract: Simple synthesis and biological activities of modafinil derivatives are described. The key reactions include condensation of acid and propargyl alcohol, subsequent 1,3-dipolar cycloaddition reaction of alkynes and (3-azido-propyl)cyclohexane or (4-azido-butyl)benzene in the presence of sodium ascorbate and CuSO₄·5H₂O in excellent yield. They were then evaluated for the suppression of LPS-induced NO generation in vitro. It was found that all compounds showed moderate effects for suppression of LPS-induced NO generation.
authors.affiliation: Department of Neuroscience and TIDRC, School of Medicine, Ewha Womans University, Seoul 158-710, Korea.
authors.forename: Jae-Chul
authors.initials: JC
authors.lastname: Jung
authors.forename: Yeonju
authors.initials: Y
authors.lastname: Lee
authors.forename: Jee-Young
authors.initials: JY
authors.lastname: Son
authors.forename: Eunyoung
authors.initials: E
authors.lastname: Lim
authors.forename: Mankil
authors.initials: M
authors.lastname: Jung
authors.forename: Seikwan
authors.initials: S
authors.lastname: Oh
mesh_terms: D000818:Animals; D001559:Benzhydryl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004952:Esters / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D017628:Microglia / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D000077408:Modafinil; D009569:Nitric Oxide / Q000378:metabolism; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D001559:Benzhydryl Compounds; D004952:Esters; D014230:Triazoles; D009569:Nitric Oxide; D000077408:Modafinil