Convenient Synthesis and Biological Evaluation of Modafinil Derivatives: Benzhydrylsulfanyl and Benzhydrylsulfinyl [1,2,3]triazol-4-yl-methyl Esters
oleh: Seikwan Oh, Mankil Jung, Eunyoung Lim, Jee-Young Son, Yeonju Lee, Jae-Chul Jung
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2011-12-01 |
Deskripsi
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 CuSO4ยท5H2O 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.