Di Braccio Mario, Grossi Giancarlo, Roma Giorgio, Piras Daniela, Mattioli Francesca, Gosmar Marzia
Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV, 3, 16132 Genova, Italy.
Eur J Med Chem. 2008 Mar;43(3):584-94. doi: 10.1016/j.ejmech.2007.04.016. Epub 2007 May 21.
On the basis of the good anti-inflammatory properties shown by the 9-alkyl-N,N-dialkyl-5-(alkylamino)[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides 1, a series of analogues of such compounds, in which the 9-alkyl substituent was replaced by an ester or amide group (compounds 3a-i), was prepared and tested (inhibition of carrageenan-induced paw edema in the rat). Also two 5-(N-alkyl,N-acylamino) derivatives (compounds 4a,b) were synthesized and evaluated for the same purpose. Even though the general trend for these new [1,2,4]triazolo[4,3-a][1,8]naphthyridine derivatives was a decrease in activity compared with compounds 1, some of the new synthesized compounds exhibited still good anti-inflammatory properties.
基于9-烷基-N,N-二烷基-5-(烷基氨基)[1,2,4]三唑并[4,3-a][1,8]萘啶-6-甲酰胺1所显示出的良好抗炎特性，制备并测试了一系列此类化合物的类似物，其中9-烷基取代基被酯基或酰胺基取代（化合物3a-i）（在大鼠中对角叉菜胶诱导的爪肿胀的抑制作用）。同样，为了相同目的合成并评估了两种5-(N-烷基,N-酰基氨基)衍生物（化合物4a,b）。尽管这些新的[1,2,4]三唑并[4,3-a][1,8]萘啶衍生物与化合物1相比活性总体呈下降趋势，但一些新合成的化合物仍表现出良好的抗炎特性。
