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Design and synthesis of carbamate and thiocarbamate derivatives and their inhibitory activities of NO production in LPS activated macrophages.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 01; Vol. 22 (9), pp. 3301-4. Date of Electronic Publication: 2012 Mar 16. - Publication Year :
- 2012
-
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 μM of IC(50). They inhibited NO production through the suppression of iNOS protein and mRNA expression and nuclear translocation of p65.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Humans
Inhibitory Concentration 50
Lipopolysaccharides pharmacology
Macrophage Activation
NF-kappa B metabolism
Nitric Oxide biosynthesis
Nitric Oxide Synthase Type II antagonists & inhibitors
Nitric Oxide Synthase Type II genetics
Structure-Activity Relationship
Carbamates chemical synthesis
Macrophages metabolism
Nitric Oxide antagonists & inhibitors
Thiocarbamates chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22475560
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.03.010