1,8-Naphthyridines VIII. Novel 5-aminoimidazo[1,2-a] [1,8]naphthyridine-6-carboxamide and 5-amino[1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamide derivatives showing potent analgesic or anti-inflammatory activity, respectively, and completely devoid of acute gastrolesivity
作者:Giorgio Roma、Mario Di Braccio、Giancarlo Grossi、Daniela Piras、Vigilio Ballabeni、Massimiliano Tognolini、Simona Bertoni、Elisabetta Barocelli
DOI:10.1016/j.ejmech.2009.10.020
日期:2010.1
interesting pharmacological properties shown by the 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamide derivatives 1, previously described by us, we have now prepared the 5-aminoimidazo[1,2-a][1,8]naphthyridine-6-carboxamide derivatives 2a–o (a new structural class) whose tricyclic system is isosteric to that of compounds 1. Both compounds 2 and some new properly substituted compounds 1 (1f–k) now
根据我们先前描述的5-氨基[1,2,4]三唑并[4,3- a ] [1,8]萘啶-6-羧酰胺衍生物1所显示的非常有趣的药理特性,我们有现在制备了5-氨基咪唑并[1,2- a ] [1,8]萘啶-6-羧酰胺衍生物2a - o(一种新的结构分类),其三环系统与化合物1的体系等排。化合物2和现在合成的一些新的适当取代的化合物1(1f - k)均已在体内进行了镇痛和抗炎活性测试:总体而言,化合物2具有明显的镇痛作用,而许多化合物1则显示出非常有效的抗炎活性,与稀少的镇痛活性相关。在大鼠中(200 mg kg -1口服剂量),所有有效化合物均被证明完全没有急性胃病(胃功能损害)。