| Autor: |
Jae-Chul Jung, Yeonju Lee, Jee-Young Son, Eunyoung Lim, Mankil Jung, Seikwan Oh |
| Předmět: |
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| Zdroj: |
Molecules; Sep2012, Vol. 17 Issue 9, p10446-10458, 13p, 4 Diagrams, 2 Graphs |
| Abstrakt: |
Simple synthesis of modafinil derivatives and their biological activity are described. The key synthetic strategies involve substitution and coupling reactions. We determined the anti-inflammatory effects of modafinil derivatives in cultured BV2 cells by measuring the inhibition of nitrite production and expression of iNOS and COX-2 after LPS stimulation. It was found that for sulfide analogues introduction of aliphatic groups on the amide part (compounds 11a-d) resulted in lower anti-inflammatory activity compared with cyclic or aromatic moieties (compounds 11e-k). However, for the sulfoxide analogues, introduction of aliphatic moieties (compounds 12a-d) showed higher anti-inflammatory activity than cyclic or aromatic fragments (compounds 12e-k) in BV-2 microglia cells. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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