Synthesis of phenylisothiourea derivatives as inhibitors of NO production in LPS activated macrophages
- Authors
- Jin, Guo Hua; Lee, Da Yeon; Cheon, Ye-Jin; Gim, Hyo Jin; Kim, Do Hee; Kim, Hee-Doo; Ryu, Jae-Ha; Jeon, 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
- Pages
- 5
- 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
1464-3405
- 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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