Synthesis and Anti‐Inflammatory Activity of Spiropyrimido[4,5‐ <i>d</i> ]pyrimidine Derivatives
Abstract Herein, we describe the high yielding synthesis of spiropyrimido[4,5‐ d ]pyrimidines by Friedländer‐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.
Authors
- Emna Maalej
- Lhassane Ismaïli (ORCID: https://orcid.org/0000-0002-6013-3150)
- Paul J. Bernard (ORCID: https://orcid.org/0000-0003-0135-3185)
- Francisco López‐Muñoz (ORCID: https://orcid.org/0000-0002-5188-6038)
- Bernard Refouvelet (ORCID: https://orcid.org/0000-0002-7939-1600)
- Jose Luis Marco-Contelles (ORCID: https://orcid.org/0000-0003-0690-0328)
- Fakher Chabchoub (ORCID: https://orcid.org/0000-0003-4375-0277)
- Olfa Kallech Ziri
- Wiem Ayadi
Institutions
- University of Sfax (TN)
- Inserm (FR)
- Research Institute Hospital 12 de Octubre (ES)
- HM Hospitales (ES)
- Instituto de Química Orgánica General (ES)
- Centre of Biotechnology of Sfax (TN)
- Université de Franche-Comté (FR)
Publication Details
- Journal
- ChemistrySelect
- Published
- 2025-04-01
- DOI
- https://doi.org/10.1002/slct.202500270
- Primary Topic
- Synthesis and biological activity
- Type
- article
- Field-Weighted Citation Impact
- 0.00