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    New silver N-heterocyclic carbenes complexes: Synthesis, molecular docking study and biological activities evaluation as cholinesterase inhibitors and antimicrobials
    (Elsevier, 2021) Lasmari, Sarra; Ikhlef, Sofiane; Boulcina, Raouf; Mokrani, El Hassen; Bensouici, Chawki; Gurbuz, Nevin; Dundar, Muhmammed
    We focused our study for the conception and the synthesis of a new series of Silver (I) N-heterocyclic carbene complexes which were obtained from the corresponding N-heterocyclic carbene (NHC) precursors and their unsymmetrical benzimidazolium salts. These new Ag-NHC complexes were screened for their antibacterial, antifungal, and anti-cholinesterase activities. The biological activities of synthesized products were compared with standard drugs. N-heterocyclic carbenes 2a-f and complexes 3a-f exhibited moderate antibacterial and antifungal activities. The results proved that the compounds indicated moderate to excellent activity against both AChE and BuChE. It was found that most of the complexes displayed good AChE and BuChE inhibitory activities. In particular, compounds 3c and 3e were the most potent inhibitors in the series with IC50 values of 8.56 +/- 1.17 mu M and 5.05 +/- 0.30 mu M against AChE and BChE, respectively. Docking studies revealed that compounds 3c and 3e bind manly to the catalytic anionic site (CAS) of the AChE, and BChE respectively. (C) 2021 Elsevier B.V. All rights reserved.
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    New Silver N-Heterocyclic Carbenes Complexes: Synthesis, Molecular Docking Study and Biological Activities Evaluation as cholinesterase inhibitors and antimicrobials (vol 1238, 130399, 2021)
    (Elsevier, 2021) Lasmari, Sarra; Ikhlef, Sofiane; Boulcina, Raouf; Mokrani, El Hassen; Bensouici, Chawki; Gurbuz, Nevin; Dundar, Muhmammed
    [Abstract Not Available]
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    Palladium (II)-N-heterocyclic Carbene Complexes: Synthesis, Molecular Docking, UV-Vis Absorption and Enzyme Inhibition
    (Bentham Science Publ Ltd, 2024) Ikhlef, Sofiane; Lasmari, Sarra; Mokrani, El Hassen; Boulcina, Raouf; Bensouici, Chawki; Gurbuz, Nevin; Ozdemir, Ismail
    Background Alzheimer's disease is the most prevalent form of dementia; it affects the brain regions responsible for thought, memory, and language. Dementia cannot currently be cured by any medication. Objective We aimed to synthesize Pd-NHC type PEPPSI and investigate their biological activity in anticholinesterase enzymes. Methods In this study, we described preparing a series of Pd-NHC type PEPPSI obtained from their unsymmetrical benzimidazolium salts. These complexes (3a-f) were synthesized from the 2-chloromethyl-1,3-dioxalane benzimidazolium salts, PdCl2, KBr and pyridine. The compounds (3a-f) were tested against two enzymes (AChE and BChE). Results The results showed that most of the Palladium-NHC complexes effectively inhibited AChE with IC50 values in the range of 4.94 - 40.03 mu M, and for BChE are in the range of 4.21 - 21.28 mu M. The results showed that the compound (3a) was the most potent inhibitor activity against both AChE and BChE. The inhibition parameter (IC50) was calculated by the spectrophotometric method. The inhibitory effects of the synthesized Pd-NHCs were compared to galantamine as a clinical cholinergic enzyme inhibitor. Additionally, Molecular docking is carried out to estimate the binding pattern between the newly synthesized compounds and both AChE and BChE active sites. Conclusion The results demonstrated that all synthesized compounds show excellent to moderate inhibition against the examined enzymes (AChE/BChE).
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    Synthesis and biological evaluation of pyrazolyl-pyrazolone derivatives: Antioxidant, anticancer activities, and molecular docking insights
    (Elsevier, 2025) Benoune, Racha Amira; Boulcina, Raouf; Dems, Mohamed Abdesselem; Ugur, Edanur; Karci, Hueseyin; Dundar, Muhammed; Koc, Ahmet
    In this study, a series of novel pyrazolyl-pyrazolone derivatives was synthesized via a Knoevenagel condensation reaction using trisodium citrate as a catalyst, highlighting an environmentally sustainable and cost-effective approach. The synthesized compounds were characterized through comprehensive analytical techniques, including NMR spectroscopy, HRMS, and melting point determination. Biological evaluations demonstrated diverse and promising activities: compound 6i exhibited exceptional antioxidant activity across DPPH, ABTS, and Ferric-phenanthroline assays, outperforming standard antioxidants like BHT and BHA. In parallel, anticancer assays against SH-SY5Y and HCT116 cell lines revealed compounds 6e, 6j, and 6k as potent cytotoxic agents, with IC50 values significantly lower than cisplatin, the reference drug. Notably, compound 6j showed remarkable selectivity towards cancer cells with reduced cytotoxicity on non-cancerous BEAS-2B cells. Molecular docking studies confirmed strong binding interactions of the active compounds with key cancer-related protein targets, shedding light on their mechanisms of action. These findings not only highlight the therapeutic potential of pyrazolyl-pyrazolone derivatives as dual antioxidant and anticancer agents but also emphasize the value of sustainable chemical processes in drug development.
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    Synthesis of [PdBr2(benzimidazole-2-ylidene)(pyridine)] complexes and their catalytic activity in the direct C-H bond activation of 2-substituted heterocycles
    (Pergamon-Elsevier Science Ltd, 2021) Lasmari, Sarra; Gurbuz, Nevin; Boulcina, Raouf; Ozdemir, Namik; Ozdemir, Ismail
    A series of unsymmetrical 1,3-disubstituted benzimidazolium chlorides, 2a-f, having two nitrogen atoms substituted by various alkyl groups were synthesized as N-heterocyclic carbene (NHC) precursors in high yields. The benzimidazolium salts are readily converted into the corresponding PEPPSI-type palladium-NHC complexes 3a-f (PEPPSI = pyridine-enhanced precatalyst preparation, stabilization and initiation). The structures of all the compounds have been characterized by H-1 NMR, C-13 NMR and IR spectroscopy, as well as the X-ray diffraction technique (3a, 3d and 3e), which support the proposed structures. Next, the palladium-NHC-PEPPSI complexes were used as catalysts in the direct C(5)-arylation of 2-acetyl furan and 2-acetylthiophene with various aryl bromides. These complexes exhibited moderate to high catalytic activities and gave C-H activation selectively at the C(5)-position of 2-acetylfuran and 2-acetylthiophene. (c) 2021 Elsevier Ltd. All rights reserved.