Parallel approach for solution-phase synthesis of 2-quinoxalinol analogues and their inhibition of LPS-induced TNF-alpha release on mouse macrophages in vitro.
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 microM (7-amino-6-[(3-methoxypropyl)amino]-3-methyl-2-quinoxalinol) and 2.2 microM (7-amino-6-[(3-butoxypropyl)amino]-3-methyl-2-quinoxalinol), respectively.
Zhang
Liang
L
Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, P. R. China.
Liu
Gang
G
Zhang
Suo-De
SD
Yang
Hong-Zhen
HZ
Li
Li
L
Wu
Xiang-Hong
XH
Yu
Junli
J
Kou
Bin-Bin
BB
Xu
Song
S
Li
Jing
J
Sun
Gang-Chun
GC
Ji
Ya-Fei
YF
Cheng
Gui-Fang
GF
D000818:Animals; D008070:Lipopolysaccharides; D008264:Macrophages; D051379:Mice; D019999:Pharmaceutical Solutions; D012996:Solutions; D014409:Tumor Necrosis Factor-alpha
D008070:Lipopolysaccharides; D019999:Pharmaceutical Solutions; D012996:Solutions; D014409:Tumor Necrosis Factor-alpha