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Simple synthesis of modafinil derivatives and their anti-inflammatory activity

Title
Simple synthesis of modafinil derivatives and their anti-inflammatory activity
Authors
Jung J.-C.Lee Y.Son J.-Y.Lim E.Jung M.Oh S.
Ewha Authors
오세관정재철
SCOPUS Author ID
오세관scopus
Issue Date
2012
Journal Title
Molecules
ISSN
1420-3049JCR Link
Citation
Molecules vol. 17, no. 9, pp. 10446 - 10458
Indexed
SCIE; SCOPUS WOS scopus
Document Type
Article
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. © 2012 by the authors.
DOI
10.3390/molecules170910446
Appears in Collections:
의과대학 > 의학과 > Journal papers
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