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Design and synthesis of urea and thiourea derivatives and their inhibitory activities on lipopolysaccharide-induced NO production

Authors
Kim, Yoon JungRyu, Jae-HaCheon, Ye JinLim, Hyo JinJeon, Raok
Issue Date
15-Jun-2007
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
urea; thiourea; carbazole; nitric oxide synthase; nitric oxide; inhibitor
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.12, pp.3317 - 3321
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
17
Number
12
Start Page
3317
End Page
3321
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/14676
DOI
10.1016/j.bmcl.2007.04.005
ISSN
0960-894X
Abstract
Series of ureas and thioureas were designed and synthesized, and their inhibitory activities of NO production in lipopolysaccharide-activated macrophages were evaluated. We found several essential moieties in the structure of the prepared compounds for the activity. Thiourea derivatives revealed higher inhibitory activity than the corresponding urea derivatives. Among these compounds, 7e having carboxymethyl group at N3 position of thiourea was the most potent in the inhibition of NO production. They inhibited NO production through the Suppression of NOS protein and mRNA expression. (c) 2007 Elsevier Ltd. All rights reserved.
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