2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2011 Apr 1;21(7):1953-7. doi: 10.1016/j.bmcl.2011.02.034.
Jieun Yoon 1,  Lan Cho,  Sang Kook Lee,  Jae-Sang Ryu
Affiliations

Affiliation

  • 1 Division of Life and Pharmaceutical Sciences, Ewha Womans University, Center for Cell Signaling and Drug Discovery Research, College of Pharmacy, 11-1 Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Republic of Korea.
PMID: 21377876 DOI: 10.1016/j.bmcl.2011.02.034
Abstract

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, 29 g showed a significant inhibitory activity (IC(50) = 12.8 μM). The inhibitory effects of 29 g on LPS-mediated NO production in macrophage cells appeared to be associated with the suppression of iNOS expression.

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