Synthesis and Anti-Inflammatory Activity of Spiropyrimido[4,5-d]pyrimidine Derivatives

被引:0
作者
Maalej, Emna [1 ]
Ziri, Olfa Kallech [2 ]
Ayadi, Wiem [2 ]
Bernard, Paul J. [3 ]
Lopez-Munoz, Francisco [4 ,5 ,6 ]
Marco-Contelles, J. [7 ]
Chabchoub, Fakher [8 ]
Refouvelet, Bernard [3 ]
Ismaili, Lhassane [3 ]
机构
[1] Ctr Biotechnol Sfax, Lab Mol & Cellular Screening Proc, POB 1177, Sfax 3018, Tunisia
[2] Inst Natl Rech & Anal Physico Chim, Lab Subst Naturelles LR10INRAP02, Ariana 2020, Tunisia
[3] Univ Franche Comte, INSERM, UMR 1322, LINC, F-25000 Besancon, France
[4] Univ Camilo Jose Cela, HM Hosp, Fac Hlth Sci, Madrid 28692, Spain
[5] HM Hosp, Hlth Res Inst, Madrid 28015, Spain
[6] Hosp 12 Octubre Res Inst, Neuropsychopharmacol Unit, Madrid 28041, Spain
[7] Inst Gen Organ Chem CSIC, C Juan De La Cierva 3, Madrid 28006, Spain
[8] Univ Sfax, Fac Sci Sfax, Lab Appl Chem Heterocycles Lipids & Polymers, BP 802, Sfax 3000, Tunisia
关键词
Anti-inflammatory agents; Biological activity; Friedlander reaction; Spiropyrimido[4,5-d] pyrimidines; Synthesis; PHARMACOLOGICAL EVALUATION; ALZHEIMERS-DISEASE; INHIBITORS; DISCOVERY; CANCER; AGENTS;
D O I
10.1002/slct.202500270
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Herein, we describe the high yielding synthesis of spiropyrimido[4,5-d]pyrimidines by Friedl & auml;nder-type reaction of substituted 4-aminopyrimidine-5-carbonitriles with cyclohexanone, using sodium ethoxide as catalyst. The biological activity of the new compounds as anti-inflammatory agents was evaluated and to predict their pharmacological properties a comprehensive in silico analysis was conducted. Among the tested compound, three compounds exhibited a potent lipoxygenase inhibitory activity comparing very well with reference octyl gallate.
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页数:5
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