Yazar "Bensouici, Chawki" seçeneğine göre listele

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  • Küçük Resim
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    Green one-pot multicomponent synthesis, biological evaluation and theoretical investigations of some novel beta-acetamido ketone derivatives as potent cholinesterase inhibitors
    (Pergamon-Elsevier Science Ltd, 2020) Chibane, Adil Ziadi; Boulcina, Raouf; Boulebd, Houssem; Bensouici, Chawki; Yıldırım, Muhammet; Debache, Abdelmadjid
    A series of novel beta-acetamido ketones have been prepared via a four-component condensation between aromatic aldehydes, enolizable ketones, acyl chloride and acetonitrile in the presence of 10 mol% of phenylboronic acid as a catalyst. The expected products have been obtained in good to excellent yields. In addition, in vitro cholinesterase inhibitory activity of title compounds has been studied and the results indicated that some compounds exhibited remarkable BChE activity. In order to gain insights into the molecular structure and chemical reactivity of the synthesized beta-acetamido ketones, density functional theory (DFT) calculations were also carried out. (C) 2020 Elsevier Ltd. All rights reserved.
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    Synthesis, molecular docking studies, and biological evaluation of novel alkyl bis(4-amino-5-cyanopyrimidine) derivatives
    (Wiley-V C H Verlag Gmbh, 2019) Boualia, Imen; Derabli, Chamseddine; Boulcina, Raouf; Bensouici, Chawki; Yıldırım, Muhammet; Yıldırım, Arzu Birinci; Mokrani, El Hassen
    A series of bis(4-amino-5-cyano-pyrimidines) was synthesized and evaluated as dual inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). To further explore the multifunctional properties of the new derivatives, their antioxidant and antibacterial activities were also tested. The results showed that most of these compounds could effectively inhibit AChE and BChE. Particularly, compound 7c exhibited the best AChE inhibitory activity (IC50 = 5.72 +/- 1.53 mu M), whereas compound 7h was identified as the most potent BChE inhibitor (IC50 = 12.19 +/- 0.57 mu M). Molecular modeling study revealed that compounds 7c, 7f, and 7b showed a higher inhibitory activity than that of galantamine against both AChE and BChE. Anticholinesterase activity of compounds 7h, 7b, and 7c was significant in vitro and in silico for both enzymes, since these compounds have hydrophobic rings (Br-phenyl, dimethyl, and methoxyphenyl), which bind very well in both sites. In addition to cholinesterase inhibitory activities, these compounds showed different levels of antioxidant activities. Indeed, in the superoxide-dimethyl sulfoxide alkaline assay, compound 7j showed very high inhibition (IC50 = 0.37 +/- 0.28 mu M). Also, compound 7l exhibited strong and good antibacterial activity against Staphylococcus epidermidis and Staphylococcus aureus, respectively. Taking into account the results of biological evaluation, further modifications will be designed to increase potency on different targets. In this study, the obtained results can be a new starting point for further development of multifunctional agents for the treatment of Alzheimer's disease.