Bulletin of the Korean Chemical Society

  • 제31권1호
  • /
  • Pages.27-30
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  • 2010
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  • 0253-2964(pISSN)
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  • 1229-5949(eISSN)
대한화학회 (Korean Chemical Society)
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Synthesis of Heterocycle-linked Thioureas and Their Inhibitory Activities of NO Production in LPS Activated Macrophages

  • Cheon, Ye-Jin (College of Pharmacy, Sookmyung Women's University) ;
  • Gim, Hyo-Jin (College of Pharmacy, Sookmyung Women's University) ;
  • Jang, Hee-Ryun (College of Pharmacy, Sookmyung Women's University) ;
  • Ryu, Jae-Ha (College of Pharmacy, Sookmyung Women's University) ;
  • Jeon, Raok (College of Pharmacy, Sookmyung Women's University)
  • 발행 : 2010.01.20
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초록

A series of thioureas were synthesized as inhibitors of NO production in lipopolysaccharide-activated macrophages. We investigated the effect of lipophilic moiety and N-substituents of the thioureas on the activity. Phenoxazine and carbazole-containing derivatives revealed higher activity than indole-containing thioureas. The appropriate spacer between lipophilic tail and thiourea head and methyl substituent at N3 position of thiourea brought beneficial effect on the inhibition of NO production. Among prepared compounds, phenoxazine-containing derivative 2a was the most potent with $2.32 {\mu}M$ of $IC_{50}$ value. RT-PCR analysis suggested that the prepared thioureas inhibited NO production through the suppression of iNOS mRNA expression.

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피인용 문헌

  1. SPA0355, a thiourea analogue, inhibits inflammatory responses and joint destruction in fibroblast-like synoviocytes and mice with collagen-induced arthritis vol.164, pp.2b, 2011, https://doi.org/10.1111/j.1476-5381.2011.01441.x
  2. ChemInform Abstract: Synthesis of Heterocycle-Linked Thiourea and Their Inhibitory Activities of NO Production in LPS Activated Macrophages. vol.41, pp.20, 2010, https://doi.org/10.1002/chin.201020146