Synthesis of phenylisothiourea derivatives as inhibitors of NO production in LPS activated macrophages
  • Guo Hua Jin
  • Da Yeon Lee
  • Ye-Jin Cheon
  • Hyo Jin Gim
  • Kim, Do Hee
  • ... Raok Jeon
  • 외 2명
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초록

A series of phenylisothioureas were synthesized as inhibitors of NO production in lipopolysaccharide-activated macrophages. We investigated the effect of lipophilic moiety and N- or S-substituents of the phenylisothioureas on the activity. Inhibitory activities of carbazole-linked phenylisothioureas were superior to the corresponding simple phenylisothiourea derivatives. Among these compounds, 12b having N- ethyl and S-isopropyl groups on phenylisothiourea moiety was the most potent in the inhibition of NO production. They inhibited NO production through the suppression of the LPS-induced translocation of p65 subunit of NF-kappa B and the followed suppression of the iNOS protein and mRNA expression. (C) 2009 Elsevier Ltd. All rights reserved.

키워드

IsothioureaNitric oxideiNOSNITRIC-OXIDE SYNTHASESELECTIVE-INHIBITIONISOFORM SELECTIVITYTHERAPEUTIC TARGETPOTENTPEROXYNITRITEISOTHIOUREASDESIGNENZYMEINOS
제목
Synthesis of phenylisothiourea derivatives as inhibitors of NO production in LPS activated macrophages
저자
Guo Hua JinDa Yeon LeeYe-Jin CheonHyo Jin GimKim, Do HeeDo Hee KimJae-Ha RyuRaok Jeon
DOI
10.1016/j.bmcl.2009.04.001
발행일
2009-06
유형
Article
저널명
Bioorganic and Medicinal Chemistry Letters
19
11
페이지
3088 ~ 3092