Facultatea de Chimie şi Tehnologie Chimică / Faculty of Chemistry and Chemical Technology
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Item SYNTHESIS AND BIOLOGICAL ACTIVITY OF N-(4-METHOXYPHENYL)-2-OXOPROPANAMIDE 4-PHENYLTHIOSEMICARBAZONE AND ITS COPPER(II) COMPLEXES(CEP USM, 2024) Graur, Ianina; Usataia, Irina; Graur, Vasilii; Tsapkov, Victor; Gulea, Aurelian; Garbuz, Olga; Balan, GretaThe new N-(4-methoxyphenyl)-2-oxopropanamide 4-phenylthiosemicarbazone (HL) and its 5 copper(II) coordination compounds [Cu(L)X] (X = Cl- (I); Br- (II); NO3- (III); CH3COO- (IV); Cl2CHCOO- (V)) have been synthesized and characterized by elemental analysis, FTIR and NMR spectra. Coordination of 4-phenylthiosemicarbazone HL with the copper(II) atom led to increased antibacterial activity against Staphylococcus aureus and Bacillus cereus. Non-coordinated 4-phenylthiosemicarbazone (HL) showed the highest activity in relation to ABTS•+ cation radicals; its activity is close to that of Trolox, which is used in medicine. The antibacterial and antioxidant activities of the synthesized complexes are influenced by the nature of the acidic residue in their composition.Item EXPLORING THE ANTIOXIDANT ACTIVITY OF 1-(PIPERIDIN-1-YL) PROPANE-1,2-DIONE 4-PHENYLTHIOSEMICARBAZONE AND 3d METAL COORDINATION COMPOUNDS WITH THIS LIGAND(CEP USM, 2024) Graur, Ianina; Maxim, Mihail; Graur, Vasilii; Tsapkov, Victor; Gulea, Aurelian; Garbuz, OlgaThe new 1-(piperidin-1-yl)propane-1,2-dione 4-phenylthiosemicarbazone (HL) and its 7 coordination compounds [Cu(L)X] (X = Br- (I); Cl- (II); NO3 - (III); CH3COO- (IV); Cl2CHCOO- (V)), [Co(L)2]NO3 (VI), [Fe(L)2]NO3 (VII) have been synthesized and characterized by elemental analysis, FTIR, 1H, 13C NMR spectra and molar electric conductibility. For the obtained compounds it was studied the antioxidant activity towards ABTS•+ radical cation. Uncoordinated 4-phenylthiosemicarbazone HL is the most active one with IC50 14.1 μM. Its activity is higher than that of Trolox which is used in medicine as an antioxidant. Among all the synthesized coordination compounds, the iron(III) complex VII showed the greatest activity. The antioxidant activity of metal complexes is influenced by the anion and the nature of the central metal atom.Item CU(II) COMPLEXES WITH 4-ALLYLTHIOSEMICARBAZONE AS POSSIBLE ANTIOXIDANT AGENTS(2022) Ulchina, Ianina; Celac, Marina; Graur, Vasilii; Tsapkov, Victor; Garbuz, Olga; Gulea, AurelianOxidation is an essential part of aerobic metabolism in living organisms. In this process, free radicals are constantly generated. It is widely known that free radicals play a dual role in vivo as both beneficial and adverse compounds. In order to maintain the balance of the activity of the free radicals in living cells, the organism has evolved antioxidant defense systems, protecting against free radical damage. However, when our endogenous defense system has incomplete efficiency, or a rise in free radicals under special conditions like smoking, chemical air pollutants, radiation, and inflammation, the imbalance between free radicals and antioxidants results in oxidative stress, which is now believed to be one of the important factors in the occurrence of certain human diseases including atherosclerosis, rheumatoid arthritis, cancer, and neurodegenerative diseases. So, the search of possible antioxidants agents is of interest, because they protect the body against damage by harmful free radicals. For this purpose two copper(II) coordination compounds of 1-(morpholin-4-yl) propane-1,2-dione 4- allylthiosemicarbazone (HL) with 1,10-phenantroline (1,10-Phen) and 2,2’-bipyridyl (2,2’- Bpy) were synthesized. On the first stage of the experiment the ethanolic solution of Cu(NO3)2⸱3H2O reacts with 4-allylthiosemicarbazone HL and on the second stage the ethanolic solution of the prepared precursor Cu(L)NO3 reacts with bidentate amines forming crystalline coordination compounds. The composition of these compounds was determined using elemental analysis for copper: Cu(1,10-Phen)(L)NO3, Cu(2,2’-Bpy)(L)NO3. The molar conductivity values of the synthesized coordination compounds are in the range 82-98 Ω- 1∙cm2∙mol-1 that indicates that these complexes are 1:1 electrolytes. A standard ABTS•+ method has been used to determine the antioxidant properties of synthesized compounds and trolox was used as a reference. The pro-ligand HL is less active than trolox, its coordination to copper(II) atom decreases antioxidant activity. The introduction of bidentate amines into the internal sphere of precursor increases the activity of complexes, that become 4 times more active than pro-ligand HL, 6 times more active than precursor, and also more active thanItem IN VITRO ANTILEUKEMIA ACTIVITY (HL-60 CELLS), OF SOME 3d METAL COMPLEXES. CHEMICAL SYNTHESIS AND STRUCTURE – ACTIVITY RELATIONSHIP(Academia de Ştiinţe a Moldovei, 2006) Gulea, Aurelian; Poirier, Donald; Roy, Jenny; Stavila, Vitalie; Bulimestru, Ion; Tsapkov, Victor; Bîrcă, Maria; Popovschi, Lilia28 years after the first approval of cisplatin in the clinic against a number of cancer diseases, cisplatin and related compounds continue to be among the most efficient anticancer drugs used so far. Efforts are focused to develop novel platinum- and non-platinum-based antitumor drugs to improve clinical effectiveness, to reduce general toxicity and to broaden the spectrum of activity. Thiosemicarbazones and their transition metal complexes demonstrated potent cytotoxic activity against a series of murine and human suspended cultured tumor cells. The aim of our communication is to report the synthesis of novel 3d metal complexes with some di- and tri-dentate ligands containing N, O and S donor atoms which have different electronic and geometrical structure confirmed by elemental and thermal analyses, molar conductance, magnetic measurements, IR and NMR data. In order to investigate the antileukemia activity 27 metal complexes were tested as inhibitors of HL60 cells growing. It was established that the nature, electronic structure and coordination number of the central atom, the geometric configuration of metal complexes and the nature of the ligands (donor atoms) are important in biological activity prediction. In investigated series of complexes the most active are those having a copper (II) or a cobalt (II) species. For the octahedral environment of the cobalt complexes the electronic configuration is important Co2+ ( 3d7 ) > Co3+ ( 3d6 ). This different activity can be explained by the fact that in solutions Co2+ complexes with inner coordination sphere lifetime of the ligands 10-4 - 10-5 s are more labile in comparison with the inert Co3+ complexes (lifetime 103 – 105 s). Copper (II) complexes with different type of electronic hybridisation and geometric structure produce also different activity. We find that a square planar Cu2+ complexes have essential activity. The activity of such square planar complexes is influenced also by the nature of the ligand donor atoms. In fact complexes with coordinated ligands containing N, O and S chelate donor atoms are essentially more active than complexes including inner sphere only nitrogen or oxygen. In this case the presence of coordinated ligand containing sulphur donor atom is indicated. If sulphur ligand donor atom is blocked by CH3 group the biological activity became unsignificant.Item SYNTHESIS, STRUCTURE AND ANTIMICROBIAL ACTIVITY OF SALICYLALDEHYDE 4-(DIMETHYLPHENYL) THIOSEMICARBAZONES AND BIOMETAL COORDINATION COMPOUNDS WITH THESE LIGANDS(Academia de Ştiinţe a Moldovei, 2017) Gulea, Aurelian; Erhan, Tatiana; Zariciuc, Elena; Petrenko, Peter; Chumakov, Yurii; Jalba, Svetlana; Tsapkov, VictorItem COPPER(II) COORDINATION COMPOUNDS WITH THIOSEMICARBAZIDE DERIVATIVES AS INHIBITORS OF SUPEROXIDE RADICALS(Marina Sokolova Publishings, 2022) Gulea, Aurelian; Tsapkov, Victor; Graur, Vasilii; Pantea, Valeriana; Andronache, Lilia; Shvets, I.; Matusovsky, V.; Lisii, D.; Botnaru, M.; Gudumac, ValentinNew biologically active coordination compounds of copper(II) based on substituted 3-(phenyl)-1-(pyridin-2-yl)prop-2-en- 1-one 4-allylthiosemicarbazones have been obtained. It was found that these compounds exhibit strong antiradical properties when interacting with a superoxide radical. Due to this property, the obtained compounds can find wide application in medicine as inhibitors of superoxide radicals in the human body, thus preventing damage of cells and tissues, multifactorial diseases, including carcinogenesis. The synthesized coordination compounds expand the arsenal of superoxide radical inhibitors with high biological activity. Their possible significance for the development of new treatment strategies for diseases associated with the overproduction of superoxide radicals discussed.Item COPPER (II) ACETATE COORDINATION COMPOUND WITH 2-FORMYLPYRIDINE 4-ALLYLTHIOSEMICARBAZONE MANIFESTS INHIBITORY ACTIVITY AGAINST SUPEROXIDE RADICALS(Marina Sokolova Publishings, 2021) Pantea, Valeriana; Graur, Vasilii; Andronache, Lilia; Gulea, Aurelian; Tsapkov, Victor; Sardari, Veronica; Gamaniuc, Mariana; Gudumac, ValentinA new biologically active coordination compound, which belongs to the class of transition metal isotiosemicarbazides - bis (2-acetate-o) -bis {[N-prop-2-en-1-yl-N'- (pyridin- 2-ylmethylidene) carbamo-hydrazonothioate] copper} dihydrate was obtained. It has established that this compound exhibits strong anti-radical properties to the action of the organic molecule with the superoxide radical. Due to this property, the obtained compound can have a wide application in medicine as an inhibitor of superoxide radicals in the human body, thus preventing damage to cells and tissues, atherosclerosis and carcinogenesis. The synthesized coordination compound expands the arsenal of superoxide radical inhibitors with high biological activity.Item COORDINATION COMPOUND, DERIVATIVE OF ISOTHIOSEMICARBAZIDE OF TRANSITION METALS AS AN INHIBITOR OF SUPEROXIDE RADICALS(2021) Pantea, Valeriana; Graur, Vasilii; Andronache, Lilia; Gulea, Aurelian; Tsapkov, Victor; Sardari, Veronica; Gamaniuc, Marina; Gudumac, ValentinA new biologically active coordination compound, which belongs to the class of transition metal isotiosemicarbazides - bis (m2-acetate-o) -bis {[N-prop-2-en-1-yl-N'- (pyridin- 2-ylmethylidene) carbamo-hydrazonothioate] copper} dihydrate was obtained. It has established that this compound exhibits strong anti-radical properties to the action of the organic molecule with the superoxide radical. Due to this property, the obtained compound can have a wide application in medicine as an inhibitor of superoxide radicals in the human body, thus preventing damage to cells and tissues, atherosclerosis and carcinogenesis. The synthesized coordination compound expands the arsenal of superoxide radical inhibitors with high biological activity.Item SYNTHESIS, STRUCTURE, AND BIOLOGICAL ACTIVITY OF MIXED-LIGAND AMINE-CONTAINING COPPER(II) COORDINATION COMPOUNDS WITH 2-(2-HYDROXYBENZYLIDENE)-N-(prop-2-en-1-yl)HYDRAZINECARBOTHIOAMIDE(Springer, 2021) Gulea, Aurelian; Ulchina, Ianina; Graur, Vasilii; Bourosh, P. N.; Smaglii, V.A.; Garbuz, Olga; Tsapkov, VictorСopper(II) nitrate reacts in ethanol with 2-(2-hydroxybenzylidene)-N-(prop-2-en-1-yl)hydrazinecarbothioamide H2L in an 1 : 1 molar ratio to form the coordination compound Cu(HL)NO3·H2O. The introduction of amines [imidazole (Im), 3,5-dibromopyridine (3,5-Br2Py), and 4-methylpyridine (4-Pic)] into the reaction mixture in a molar ratio 1 : 1 : 2 leads to the formation of CuA(HL)NO3·nH2O [A = Im, 3,5-Br2Py, 4-Pic; n = 0, 3] complexes. The structure of the obtained compounds was determined by X-ray structural analysis. The synthesized complexes exhibit antimicrobial, antifungal, antioxidant, and anticancer activities.Item SYNTHESIS AND BIOLOGICAL ACTIVITY OF NICKEL AND COPPER COORDINATION COMPOUNDS OF 5-NITROFURAN-2-CARBALDEHYDE N(4)-ALLYL-3-THIOSEMICARBAZONE(CEP USM, 2014) Graur, Vasilii; Zariciuc, Elena; Tsapkov, Victor; Barba, Nina; Gulea, AurelianThe paper presents the synthesis of the ligand 5-nitrofuran-2-carbaldehyde N(4)-allyl-3-thiosemicarbazone (HL) and eight coordination compounds of copper(II) and nickel(II) with this ligand. The structure of thiosemicarbazone HL was studied using 1 H and 13С NMR spectroscopy. For the synthesized compounds their antimicrobial and antifungal activity was studied on a series of standard strains. For HL and Cu(HL)2(NO3)2 the antitumor activity towards human leukemia HL-60 cells was estimated. It was established that coordination compounds manifest better activity than free ligand.