title: Design and synthesis of carbamate and thiocarbamate derivatives and their inhibitory activities of NO production in LPS activated macrophages.
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.
authors.affiliation: Research Center for Cell Fate Control, College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Ku, Seoul 140-742, Republic of Korea.
authors.forename: Guo Hua
authors.initials: GH
authors.lastname: Jin
authors.forename: Hwa Jin
authors.initials: HJ
authors.lastname: Lee
authors.forename: Hyo Jin
authors.initials: HJ
authors.lastname: Gim
authors.forename: Jae-Ha
authors.initials: JH
authors.lastname: Ryu
authors.forename: Raok
authors.initials: R
authors.lastname: Jeon
mesh_terms: D002219:Carbamates / Q000138:chemical synthesis*; D006801:Humans; D020128:Inhibitory Concentration 50; D008070:Lipopolysaccharides / Q000494:pharmacology; D008262:Macrophage Activation; D008264:Macrophages / Q000378:metabolism*; D016328:NF-kappa B / Q000378:metabolism; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors / Q000235:genetics; D013329:Structure-Activity Relationship; D013859:Thiocarbamates / Q000138:chemical synthesis*
chemical_list: D002219:Carbamates; D008070:Lipopolysaccharides; D016328:NF-kappa B; D013859:Thiocarbamates; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II