Syntheses of 1,2,3-triazolyl salicylamides with inhibitory activity on lipopolysaccharide-induced nitric oxide production

Syntheses of 1,2,3-triazolyl salicylamides with inhibitory activity on lipopolysaccharide-induced nitric oxide production

A 28-membered 1,2,3-triazolyl salicylamide library was synthesized via a click chemistry. Compound 29g inhibited NO production in LPS-activated RAW264.7 macrophage cells with the IC 50 value of 12.8 μM. A 28-membered 1,2,3-triazolyl salicylamide library was synthesized via a Cu(I)-catalyzed azide-al...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (7), p.1953-1957
Hauptverfasser: Yoon, Jieun, Cho, Lan, Lee, Sang Kook, Ryu, Jae-Sang
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cell Line
Click chemistry
copper
inducible nitric oxide synthase
Inhibitory Concentration 50
iNOS
Library
Lipopolysaccharides - pharmacology
macrophages
Medical sciences
Mice
nitric oxide
Nitric Oxide - antagonists & inhibitors
Nitric Oxide - biosynthesis
Nitric Oxide Synthase Type II - antagonists & inhibitors
Nitric Oxide Synthase Type II - metabolism
Pharmacology. Drug treatments
Salicylamide
Salicylamides - chemical synthesis
Salicylamides - pharmacology
Triazole
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Zusammenfassung:A 28-membered 1,2,3-triazolyl salicylamide library was synthesized via a click chemistry. Compound 29g inhibited NO production in LPS-activated RAW264.7 macrophage cells with the IC 50 value of 12.8 μM. A 28-membered 1,2,3-triazolyl salicylamide library was synthesized via a Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition and evaluated for their abilities to inhibit NO production in LPS-activated RAW264.7 macrophage cells. Among 28 analogues, 29g showed a significant inhibitory activity (IC 50 = 12.8 μM). The inhibitory effects of 29g on LPS-mediated NO production in macrophage cells appeared to be associated with the suppression of iNOS expression.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.02.034