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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
vol. 17, no. 9, pp. 10446 - 10458
Indexed
SCIE; SCOPUS WOS scopus
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:
의학전문대학원 > 의학과 > Journal papers
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