一些新型环取代的3-苯基-1-(1,4-二氮氧化物喹喔啉-2-基)-2-丙烯-1-酮衍生物及其4,5-二氢-(1H)-吡唑类似物的合成与抗炎/抗氧化活性
Synthesis and anti-inflammatory/antioxidant activities of some new ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives and of their 4,5-dihydro-(1H)-pyrazole analogues.
作者信息
Burguete Asunción, Pontiki Eleni, Hadjipavlou-Litina Dimitra, Villar Raquel, Vicente Esther, Solano Beatriz, Ancizu Saioa, Pérez-Silanes Silvia, Aldana Ignacio, Monge Antonio
机构信息
Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain.
出版信息
Bioorg Med Chem Lett. 2007 Dec 1;17(23):6439-43. doi: 10.1016/j.bmcl.2007.10.002. Epub 2007 Oct 5.
We report the synthesis, anti-inflammatory and antioxidant activities of novel ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives and of their 4,5-dihydro-(1H)-pyrazole analogues. The tested compounds inhibit the carrageenin-induced rat paw edema (4.5-56.1%) and present important scavenging activities. Compound 2a is the most potent (56.1%) in the in vivo experiment and exhibits promising in vitro inhibition of soybean lipoxygenase (IC(50)<1microM).
我们报道了新型环取代的3-苯基-1-(1,4-二氮氧化物喹喔啉-2-基)-2-丙烯-1-酮衍生物及其4,5-二氢-(1H)-吡唑类似物的合成、抗炎和抗氧化活性。所测试的化合物可抑制角叉菜胶诱导的大鼠足爪水肿(4.5 - 56.1%)，并具有重要的清除活性。化合物2a在体内实验中活性最强(56.1%)，并且在体外对大豆脂氧合酶表现出有前景的抑制作用(IC(50)<1μM)。
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