Synthèse et caractérisation de nouveaux dérivés de B-énaminones et de sulfamides, étude théorique et activité biologique

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2024
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The work presented in this manuscript lies on two specific families of compounds that shows versatility in both reactivity and pharmacology; B-enaminones and sulfamides.B-enaminone derivatives were utilized as precursors to three different sets of compounds bearing respectively the B-enaminocarboxamide, the 4-hydroxyquinolone, and the acridine cores.Synthetic procedures were elaborated and optimized for the three series, in order to give final products in the most improved aspect. Microwave irradiation was employed in the synthesis of 4- hydrooxyquinolone and acridine analogues. On the other hand, a sulfamide-based small set of compounds was synthesized using sulfanilamide as a starting material.All synthesized mpounds were subjected to characterization using IR, NMR, LC-MS, and X-ray diffraction analysis to provide all the needed structural information. In vitro studies were conducted to the synthesized molecules including antioxidant tests according to DPPH and ABTS assays for all compounds, as well as the antidiabetic evaluation through B-amylase inhibition B- aminocarboxamides. In silico investigations were accomplished as a complementary study including molecular docking simulation, density functional theory DFT study, and ADME prediction.
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