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1

Department of Neuroscience and Tissue Injury Defense Research Center, School of Medicine, Ewha Womans University, Seoul 158-710, Korea

2

Department of Chemistry, Yonsei University, Seoul 120-749, Korea





*

Author to whom correspondence should be addressed.



Abstract 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.

Keywords: modafinil; anti-inflammation; nitric oxide; S-alkylation; coupling reaction modafinil; anti-inflammation; nitric oxide; S-alkylation; coupling reaction





Autor: Jae-Chul Jung 1, Yeonju Lee 1, Jee-Young Son 2, Eunyoung Lim 2, Mankil Jung 2 and Seikwan Oh 1,*

Fuente: http://mdpi.com/



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