title: Benzothiazolium compounds: novel classes of inhibitors that suppress the nitric oxide production in RAW264.7 cells stimulated by LPS/IFNgamma.
abstract: A series of benzothiazolium compounds were identified as novel classes of inhibitors of nitric oxide production in a cell culture system. They exhibited approximately 1600 folds potency with IC(50) at approximately 50nM to several microM as compared to IC(50) 88.4microM of l-NMMA, a known inhibitor of nitric oxide synthase. The mechanistic studies suggest that decreased iNOS protein synthesis and mRNA transcription, at least in part, were related to the inhibitory activity of effective benzothiazolium compounds. The correlation of in vivo and in vitro activities using mouse paw edema model was also demonstrated.
authors.affiliation: Division of Biotechnology and Pharmaceutical Researches, National Health Research Institutes, 35, Keyan Road, Zhunan Town, Miaoli County, Taiwan, ROC.
authors.forename: Huan-Yi
authors.initials: HY
authors.lastname: Tseng
authors.forename: Ssu-Hui
authors.initials: SH
authors.lastname: Wu
authors.forename: Wen-Hsin
authors.initials: WH
authors.lastname: Huang
authors.forename: Shao-Fang
authors.initials: SF
authors.lastname: Wang
authors.forename: Yung-Ning
authors.initials: YN
authors.lastname: Yang
authors.forename: Neeraj
authors.initials: N
authors.lastname: Mahindroo
authors.forename: Tsu
authors.initials: T
authors.lastname: Hsu
authors.forename: Weir-Torn
authors.initials: WT
authors.lastname: Jiaang
authors.forename: Shiow-Ju
authors.initials: SJ
authors.lastname: Lee
mesh_terms: D000818:Animals; D052160:Benzothiazoles; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D007371:Interferon-gamma / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D051379:Mice; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D052160:Benzothiazoles; D004791:Enzyme Inhibitors; D008070:Lipopolysaccharides; D013844:Thiazoles; D009569:Nitric Oxide; D007371:Interferon-gamma; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse; C005465:benzothiazole