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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzhydryl Compounds / chemical synthesis*
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Benzhydryl Compounds / chemistry
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Benzhydryl Compounds / pharmacology*
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Cell Line
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Esters / chemical synthesis
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Esters / chemistry
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Esters / pharmacology
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Mice
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Microglia / cytology
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Microglia / drug effects
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Microglia / metabolism
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Modafinil
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Nitric Oxide / metabolism
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacology*
Substances
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Benzhydryl Compounds
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Esters
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Triazoles
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Nitric Oxide
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Modafinil