Publications Scientifiques

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Author: search.filters.author.Makhloufi-Chebli, MalikaSubject: search.filters.subject.Antibacterial activity

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    Green synthesis, antioxidant and antibacterial activities of 4-aryl-3,4- dihydropyrimidinones/thiones derivatives of curcumin. Theoretical calculations and mechanism study
    (Elsevier, 2019) Khaldi-Khellafi, Nassima; Makhloufi-Chebli, Malika; Oukacha-Hikem, Djamila; Terachet Bouaziz, Souhila; Ould Lamara, Kamilia; Idir, Taous; Benazzouz-Touami, Amina; Dumas, Françoise
    3,4-Dihydropyrimidin-2(1H)-one/thione analogs of curcumin were synthesized in good yield by a onepot multi-component cyclocondensation using curcumin, substituted aromatic aldehydes, and urea/ thiourea in less volume of ethanol catalysed by commercial heteropolyacide Keggin type H3PMo12O40 5% mol as a recyclable and nontoxic catalyst under conventional heating and microwave irradiation. All the synthesized curcumin derivatives 4aen were screened for antioxidant and antimicrobial activity. Biological activity data of the synthesized showed that most of the synthesized compounds exhibited greater antioxidant and antibacterial activity than curcumin. Geometries of synthesized compounds were optimized by using B3LYP method with 6-31G* basis set. Then, DFT based reactivity descriptors such as HOMO, LUMO, chemical hardness, electronegativity, chemical potential were calculated and discussed.
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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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    Transition-metal complexes of N,N′-di(4-bromophenyl)-4-hydroxycoumarin-3-carboximidamide : synthesis, characterization, biological activities, ADMET and drug-likeness analysis
    (Elsevier, 2021) Belkhir-Talbi, Drifa; Ghemmit-Doulache, Naima; Terrachet-Bouaziz, Souhila; Makhloufi-Chebli, Malika; Rabahi, Amal; Ismaili, Lhassane; Silva, Artur M.S.
    Coordination compounds of N,N’-di(4-bromophenyl)-4-hydroxycoumarin-3-carboximidamide (L1) were synthesized via the reaction of Cu (II), Co (II) and Zn (II) salts in molar ratio 1 : 1 in the presence of ammoniac as basic media. The Ligands and the complexes formed were characterized using FT-IR, UV–visible and fluorescence spectrophotometric analyses, mass spectrometry, elemental analyses and NMR spectroscopy. It was concluded that N,N’-di(4-bromophenyl)-4-hydroxycoumarin-3-carboximidamide (L1) coordinated as a mono ligand for all the complexes; it also coordinated via the –OH and –NH groups. The electrochemical behaviour of these compounds was determined by cyclic voltammetry. The synthesized compounds were screened for their antimicrobial and antioxidant activities. All the complexes except that of copper show good activities against the S. aureus and those of cobalt and zinc have very interesting diameters of inhibition but lower antioxidant activity than the ligand L1. Parameters drug-likeness and ADMET (Absorption, Distribution, Metabolism, and Excretion) properties have been calculated