Styrylheterocycles: a novel class of inhibitors on lipopolysaccharide-Induced nitric oxide production.
A series of styrylheterocycles was prepared and their inhibitory activities against nitric oxide (NO) production were evaluated in a cell culture system using lipopolysaccharide-stimulated RAW264.7 macrophage cells. Our studies have identified a new series of inhibitors on NO production, providing the basis for further development of potent inhibitors. The preliminary structure-activity relationship, to elucidate the essential structural requirements, has been described. Mechanistic studies suggest that the suppression of iNOS mRNA transcription is, at least in part, related to the inhibitory activity of styrylheterocycles.
Lee
Sang Kook
SK
College of Pharmacy, Ewha Womans University, 11-1 Daehyun, Seodaemun, Seoul 120-750, South Korea.
Min
Hye Young
HY
Huh
Sun Kyung
SK
Kim
Eun-Young
EY
Lee
Eunjung
E
Song
Soyoung
S
Kim
Sanghee
S
D000818:Animals; D002478:Cells, Cultured; D017931:DNA Primers; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000201:enzymology; D051379:Mice; D009569:Nitric Oxide / Q000096:biosynthesis*; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors* / Q000096:biosynthesis / Q000235:genetics; D052247:Nitric Oxide Synthase Type II; D012333:RNA, Messenger / Q000096:biosynthesis; D020133:Reverse Transcriptase Polymerase Chain Reaction; D013329:Structure-Activity Relationship; D013343:Styrenes / Q000138:chemical synthesis* / Q000494:pharmacology*
D017931:DNA Primers; D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D008070:Lipopolysaccharides; D012333:RNA, Messenger; D013343:Styrenes; D009569:Nitric Oxide; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse