作者:Frazier, Théo、Murail, Pauline、Boulangé, Arthur、Chalane, Nazim、Giraud, Francis、Artola, Alain、Dallel, Radhouane、Anizon, Fabrice、Moreau, Pascale
DOI:10.1039/d4md00375f
日期:——
A series of 3,5-disubtituted pyridin-2(1H)-ones was synthesized. As part of a structure–activity relationship study performed in this series, structural modifications were based on 3-(indol-4-yl)-5-(pyridin-4-ylamino)pyridin-2(1H)-one B, which exhibited a potent anti-allodynic effect in a rat model of inflammatory pain. In this study, new compounds were assessed for their ability to inhibit cutaneous
合成了一系列3,5-二取代的吡啶-2( 1H )-酮。作为本系列中进行的构效关系研究的一部分,结构修饰基于 3-(indol-4-yl)-5-(pyridin-4-ylamino)pyridin-2(1 H )-one B ,在炎症性疼痛大鼠模型中表现出有效的抗异常疼痛作用。在这项研究中,通过使用辣椒素疼痛模型评估了新化合物抑制大鼠皮肤机械异常性疼痛的能力。化合物36是一种 2-甲氧基吡啶衍生物,产生了最有希望的结果,显示出增强的镇痛效果。