Parallel approach for solution-phase synthesis of 2-quinoxalinol analogues and their inhibition of LPS-induced TNF-α release on mouse macrophages in vitro

被引：31

作者：

Zhang, LA

Liu, G

Zhang, SD

Yang, HZ

Li, L

Wu, XH

Yu, JL

Kou, BB

Xu, S

Li, J

Sun, GC

Ji, YF

Cheng, GF

机构：

[1] Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China

[2] Peking Union Med Coll, Beijing 100050, Peoples R China

来源：

JOURNAL OF COMBINATORIAL CHEMISTRY | 2004年 / 6卷 / 03期

关键词：

D O I：

10.1021/cc034035h

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A parallel solution-phase synthesis of 2-quinoxalinol analogues is described. The key step-simultaneous reductions of m-Ar(NO2)(2) to m-Ar(NH2)(2) was investigated extensively. We obtained preliminary pharmacological activity of those analogues for the inhibition of LPS-induced TNF-alpha release on mouse macrophage in vitro. Two compounds revealed inhibitory activity, with IC50 values of 0.40 muM (7-amino-6-[(3-methoxypropyl)amino]-3-methyl-2-quinoxalinol) and 2.2 muM (7-amino-6-[(3-butoxypropyl)amino]-3-methyl-2-quinoxalinol), respectively.

引用

页码：431 / 436

页数：6

共 13 条

[1] Parallel approach for solution-phase synthesis of 2-quinox-alinol analogues and their inhibition of LPS-induced TNF-α release on mouse macrophages in vitro (vol 6, pg 431, 2004)
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[2] Solution-phase reductive cyclization of 2-quinoxalinol analogs: Systematic study of parallel synthesis
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[3] Solution-phase reductive cyclization of 2-quinoxalinol analogs: Systematic study of parallel synthesis
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[4] An efficient method for solution-phase parallel synthesis of 2-quinoxalinol salen schiff-base ligands
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[7] The A2A adenosine receptor inhibits LPS-induced TNF-α release from murine peritoneal macrophages through a PKA-independent pathway
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[8] Effect of retinoids on LPS-induced COX-2 expression and COX-2 associated PGE2 release from mouse peritoneal macrophages and TNF-α release from rat peripheral blood mononuclear cells
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TOXICOLOGY LETTERS, 2004, 150 (02) : 191 - 201
[9] Synthesis of unsymmetrical monocarbonyl curcumin analogues with potent inhibition on prostaglandin E2 production in LPS-induced murine and human macrophages cell lines
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[10] Effect of retinoids on LPS-induced COX-2 expression and COX-2 associated PGE2 releasing from mouse peritoneal macrophages and TNF-α release from rat periphaeral blood mononuclear cells
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