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Synthesis of phenylisothiourea derivatives as inhibitors of NO production in LPS activated macrophages

Authors
Jin, Guo HuaLee, Da YeonCheon, Ye-JinGim, Hyo JinKim, Do HeeKim, Hee-DooRyu, Jae-HaJeon, Raok
Issue Date
1-Jun-2009
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Isothiourea; Nitric oxide; iNOS
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.19, no.11, pp.3088 - 3092
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
19
Number
11
Start Page
3088
End Page
3092
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/13737
DOI
10.1016/j.bmcl.2009.04.001
ISSN
0960-894X
Abstract
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.
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