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Design and synthesis of carbamate and thiocarbamate derivatives and their inhibitory activities of NO production in LPS activated macrophages
- Authors
- Jin, Guo Hua; Lee, Hwa Jin; Gim, Hyo Jin; Ryu, Jae-Ha; Jeon, Raok
- Issue Date
- 1-May-2012
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Carbamate; Thiocarbamate; Nitric oxide; iNOS
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.22, no.9, pp 3301 - 3304
- Pages
- 4
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 22
- Number
- 9
- Start Page
- 3301
- End Page
- 3304
- ISSN
- 0960-894X
1464-3405
- Abstract
- Series of carbamate and thiocarbamate derivatives were designed and synthesized and their inhibitory activities of NO production in lipopolysaccharide-activated macrophages were evaluated. Several thoicarbamate derivatives revealed promising inhibitory activity. The structure-activity relationship study of these compounds is also reported. Among these compounds, compound 12b was the most potent with 6.5 mu M of IC50. They inhibited NO production through the suppression of iNOS protein and mRNA expression and nuclear translocation of p65. (C) 2012 Elsevier Ltd. All rights reserved.
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