Efficient Two-Step Synthesis of Novel Pyrimido[4,5-d] Pyrimidines with Potent Neuroprotective, Antioxidant, and Aβ Anti-Aggregation Properties

Eleven new differently substituted N,7-diphenylpyrimido [4,5-d]pyrimidin-4-amines 4a–k were synthesized from readily available reagents in a simple and inexpensive two-step procedure with yields up to 57%. Neuroprotective analysis against H2O2 and analysis using ORAC assays identified compounds 4g,...

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Bibliographic Details
Authors: Ghada Ben, Ameur, Maalej, Emna, Martin, Helene, Jacquinot, Anne-Sophie, Barbanneau, Nadine, Bernard, Paul J., Marco-Contelles, José, Chabchoub, Fakher, Ismaili, Lhassane
Format: article
Status:Published version
Publication Date:2024
Country:España
Institution:Consejo Superior de Investigaciones Científicas (CSIC)
Repository:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/370213
Online Access:http://hdl.handle.net/10261/370213
Access Level:Open access
Keyword:Aβ1-42 self-aggregation inhibition
antioxidant
neuroprotective agents
pyrimido [4,5-d] pyrimidines
Description
Summary:Eleven new differently substituted N,7-diphenylpyrimido [4,5-d]pyrimidin-4-amines 4a–k were synthesized from readily available reagents in a simple and inexpensive two-step procedure with yields up to 57%. Neuroprotective analysis against H2O2 and analysis using ORAC assays identified compounds 4g, 4i and 4j as promising antioxidant compounds. These compounds also showed potent inhibition of Aβ1–42 self-aggregation, and suitable physicochemical properties predicted by Datawarior software V6.1.0, this biological activity and physicochemical property being of great interest for pathologies linked to oxidative stress, such as Alzheimer’s disease.