Publications Scientifiques

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    Synthesis, characterization, theoretical studies, ADMET and drug- Likeness analysis: Electrochemical and biological activities of metal complexes of 3-(2-hydroxybenzoyl)-2H-chromen-2-one
    (Elsevier, 2019) Belkhir-Talbi, Drifa; Makhloufi-Chebli, Malika; Terrachet-Bouaziz, Souhila; Hikem-Oukacha, Djamila; Ghemmit, Naima; Ismaili, Lhassane; M.S Silva, Artur; Maamar, Hamdi
    Coordination compounds of 3-(2-hydroxybenzoyl)-2H-chromen-2-one were synthesized by the reaction of Cu(II), Co(II) and Zn(II) salts in molar ratio 1: 1 in basic media. The compounds formed were characterized using infrared, Uv–vis spectrophotometric analyses, mass spectrometry, elemental analyses and NMR spectroscopy. It was concluded that 3-(2-hydroxybenzoyl)-2H-chromen-2-one coordinated as a mono ligand for all the complexes; it also coordinated via the two carbonyl moieties. The electrochemical behavior of these compounds was determined by cyclic voltammetry. The synthesized compounds were screened for their antimicrobial and antioxidant activities. The complexes exhibited good antimicrobial activity against Staphylococcus aureus (ATCC 25923) and good antioxidant activity. Parameters drug-likeness and ADME properties are calculated.
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    Synthesis, biological activities and molecular docking study of 3-(3-oxobutanoyl)-2H-chromen-2-one derivative
    (Elsevier, 2021) Benazzouz-Touami, Amina; Hikem-Oukacha, Djamila; Ould Lamara, Kamilia; Halit, Sabrina; Terrachet-Bouaziz, Souhila; Makhloufi-Chebli, Malika
    Herein, we report the highly efficient total synthesis of a series of 3-(3-oxobutanoyl)-2H-chromen-2-one derivatives from salicylaldehyde(s) and 4‑hydroxy-6-methyl-2H-pyran-2-one (TAL) using Na2S2O3 as green and efficient catalyst. Structure elucidation of the products has been accomplished based on FT-IR, mass spectroscopy, 1H NMR and 13C NMR spectroscopy. The in vitro antioxidant activities of the drugs 3-(3-oxobutanoyl)-2H-chromen-2-one were tested by the quantitative 1,1-diphenyl-2-picrylhydrazyl (DPPH.) radical scavenging activity method. The compounds 3b, 3c and 3e proved to be the most active, showing high capacity to deplete the DPPH radicals. All synthesized compounds were screened for their antimicrobial activities and the results show that only 3f was active against bacteria Staphylococcus aureus compared to antibiotic used as reference. In addition, all synthesized compounds were docked with FtsZ from S. aureus protein using AutoDock 4 software. The results suggest that 3f binds with FtsZ protein with lower energy and undergoes good interactions with the active site amino
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    Selectivity control in the reaction between 2-hydroxyarylaldehydes and 4-hydroxycoumarin. Antioxidant activities and computational studies of the formed products
    (Elsevier, 2021) Ould Lamara, Kamilia; Makhloufi-Chebli, Malika; Benazzouz-Touami, Amina; Terrachet-Bouaziz, Souhila; Hamdi, Nejla; Silva, Artur M.S.; Behr, Jean-Bernard
    A series of 6H,7H-7-(4-Hydroxy-3-coumarinyl)[1]benzopyrano[4,3-b][1]benzopyran-6-ones 4a-g and 3-(2-hydroxybenzoyl)-2H-chromen-2-ones 5a-g derivatives were synthesized by reaction of 4-hydroxycoumarin with 2-hydroxyarylaldehydes 2a-f or 2-hydroxynaphtaldehyde 2g using different solvents and acid/base catalysts. The approach relies on a regioselective cascade reaction involving one/two molar equiv of the 4-hydroxy coumarin iteratively acting as active methylene substrate in a Knoevenagel condensation and in a Michael addition. The structures of all compounds were established by IR, mass spectrometry, 1H-NMR and 13C-NMR. Antioxidant activity of the synthesized compounds were determined using the DPPH scavenging assay, best results being obtained with 5b (IC50 = 236 µg/mL). Computational studies showed that the compounds bind in the ATP-binding site of p38 MAPK, in a same manner than known polyaromatic potent inhibitors. The synthesized compounds might be considered further for cancer therapy