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Öğe Copper-catalyzed azide-alkyne cycloaddition (CuAAC) under mild condition in water: Synthesis, catalytic application and biological activities(Elsevier Science Sa, 2017) Touj, N.; Chakchouk-Mtibaa, A.; Mansour, L.; Harrath, A. H.; Al-Tamimi, J. H.; Ozdemir, I.; Mellouli, L.A series of Cu-N-heterocyclic carbene (Cu-NHC) complexes, 3a-c, were synthesized and characterized by spectroscopic methods such as NMR, HRMS and elemental analysis. The performance of these (Cu-NHC) complexes, 3a-c showed excellent activity in 1,3-dipolar cycloaddition reactions between alkynes and azides to obtain 1,4-disubstituted triazoles 6a-d in 80%-91% isolated yields. All obtained complexes especially compounds 3a and 3c, presented significant inhibitory activity against the tested food-borne pathogens and clinical microorganisms. The compound 3a presents against S. aureus a MIC value of 4.8 mg/ml quite similar to that of ampicillin (4 mg/ml) used as standard. Compounds 3a and 3b, from a concentration of 0.5 mg/ml, present an identical scavenging activity to that of the two used controls butylated hydroxytoluene (BHT) and gallic acid (GA). Concerning acetylcholinesterase inhibition activity (AChEI), compound 6a presents an interesting AChEI activity with 68.3% of inhibition. (C) 2017 Published by Elsevier B.V.Öğe Ru(ii)-N-heterocyclic carbene complexes: synthesis, characterization, transfer hydrogenation reactions and biological determination(Royal Soc Chemistry, 2019) Boubakri, Lamia; Chakchouk-Mtibaa, A.; Al-Ayed, Abdullah S.; Mansour, L.; Abutaha, Nael; Harrath, Abdel Halim; Mellouli, L.A series of ruthenium(ii) complexes with N-heterocyclic carbene ligands were successfully synthesized by transmetalation reactions between silver(i) N-heterocyclic carbene complexes and [RuCl2(p-cymene)](2) in dichloromethane under Ar conditions. All new compounds were characterized by spectroscopic and analytical methods. These ruthenium(ii)-NHC complexes were found to be efficient precatalysts for the transfer hydrogenation of ketones by using 2-propanol as the hydrogen source in the presence of KOH as a co-catalyst. The antibacterial activity of ruthenium N-heterocyclic carbene complexes 3a-f was measured by disc diffusion method against Gram positive and Gram-negative bacteria. Compounds 3d exhibited potential antibacterial activity against five bacterial species among the six used as indicator cells. The product 3e inhibits the growth of all the six tested microorganisms. Moreover, the antioxidant activity determination of these complexes 3a-f, using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2 '-azinobis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS) as reagent, showed that compounds 3b and 3d possess DPPH and ABTS antiradical activities. From a concentration of 1 mg ml(-1), these two complexes presented a similar scavenging activity to that of the two used controls gallic acid (GA) and butylated hydroxytoluene (BHT). From a concentration of 10 mg ml(-1), the percentage inhibition of complexes 3b and 3d was respectively 70% and 90%. In addition, these two Ru-NHC complexes exhibited antifungal activity against Candida albicans. Investigation of the anti-acetylcholinesterase activity of the studied complexes showed that compounds 3a, 3b, 3d and 3e exhibited good activity at 100 mu g ml(-1) and product 3d is the most active. In a cytotoxicity study the complexes 3 were evaluated against two human cancer cell lines MDA-MB-231 and MCF-7. Both 3d and 3e complexes were found to be active against the tested cell lines showing comparable activity with examples in the literature.Öğe Synthesis, characterization, biological determination and catalytic evaluation of ruthenium(ii) complexes bearing benzimidazole-based NHC ligands in transfer hydrogenation catalysis(Royal Soc Chemistry, 2020) Slimani, Ichraf; Chakchouk-Mtibaa, A.; Mansour, L.; Mellouli, L.; Ozdemir, I; Gurbuzd, Nevin; Hamdi, NaceurA new series of ruthenium(ii) N-heterocyclic carbene complexes has been synthesized via transmetalation. These complexes are easily handled in very good yields via synthesis of silver-NHC complexes and subsequent reaction with [RuCl2(p-cymene)](2) in dichloromethane (DCM) under argon atmosphere. The new ruthenium(ii)-NHC complexes were applied to transfer hydrogenation of ketone derivatives using 2-propanol as a hydrogen source and KOH as a co-catalyst. The results show that the corresponding alcohols could be obtained in good yield with high catalyst activity (up to 76%) under mild conditions. All new compounds were characterized by spectroscopic and analytical methods. The antibacterial activities of the corresponding ruthenium(ii)-NHC complexes 4a-i were tested against positive and negative bacteria using the agar dilution procedure and their IC50 values have been determined. A cytotoxicity study of the ruthenium(ii)-NHC complexes 4 was performed against the two human cancer cell lines MDA-MB-231 and MCF-7. In addition, the scavenging activity of the synthesized complexes for the DPPH radical was also determined.Öğe Synthesis, spectroscopic properties and biological activity of new Cu(I) N-Heterocyclic carbene complexes(Elsevier, 2019) Touj, N.; Chakchouk-Mtibaa, A.; Mansour, L.; Harrath, A. H.; Al-Tamimi, J.; Mellouli, L.; Ozdemir, INew benzimidazolium salts (2) and their copper N-heterocyclic carbene complexes (3 4) were designed, synthesized and structurally characterized by NMR (H-1 and C-13), IR, HRMS and elemental analysis. All obtained complexes especially compounds 3d and 3e, presented significant inhibitory activity against the tested food-borne pathogens and clinical microorganisms. The compound 3b presents against S. aureus a MIC value of 0.0195 mg/ml quite similar to that of ampicillin (0.0195 mg/ml) used as standard. Compounds 3a and 3b, from a concentration of 0.5 mg/ml, present an identical scavenging activity to that of the two used controls butylated hydroxytoluene (BHT) and gallic acid (GA). Concerning acetylcholinesterase inhibition activity (AChEI), compound 3e presents an interesting AChEI activity with 32.80% of inhibition. (C) 2018 Published by Elsevier B.V.
