Browsing by Author "Lozan-Tîrșu, Carolina"
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Item AROMATIC ISOTHIOCYANATOPROPENONES AND THIOUREA DERIVATIVES. SYNTHESIS AND BIOLOGICAL PROPERTIES(2014) Barba, Nicanor; Gulea, Aurelian; Popușoi, Ana; Lozan-Tîrșu, Carolina; Poirier, DonaldÎn prezenta lucrare se descriu metode de sinteză a unor propenone aromatice cu grupe tioamidice sau izotiocian şi caracteristica lor biologică in vitro. Prin condensarea în cataliză acidă sau bazică a 4-(dimetilamino)benzaldehidei 4-Hidroxi-3-metoxibenzaldehidei şi furan-2-carbaldehidei cu 3-(4-acetilfenil)-1,1dimetiltioureea au fost obţinute propenone aromatice cu grupări –NHCSN(CH3)2, care la tratare termică sau în prezenţă de agenţi cu caracter acid (HCl, H2SO4, (CH3CO)2O, CH3COCl) elimină dimetilamină, transformîndu-se în izotiocianato -propenon cu randamentul de 54-92 %. La tratarea izotiocianatopropenonelor cu amine primare au fost obţinuti derivaţi cu grupări tioamidice-NHCSNH. Structura compuşilor noi obţinuţi cu conţinut de sulf a fost confirmată prin analiză elementală şi spectrală IR, 1H-, 13C- RMN. Compuşii sintetizaţi au fost testaţi ca inhibitori ai proliferării celulelor leucemice (HL-60), iar pentru produşii care au manifestat proprietăţi mai ponunţate, a fost testată in vitro activitatea lor antibacteriană faţă de unele microorganisme gram-pozitive şi gram-negative: Escherichia coli, Staphylococcus aureus, Shigella sonnei, Salmonella abony şi Bacillus cereus.Item COORDINATION COMPOUNDS OF COPPER WITH 2-FORMYLPYRIDINE 4-(DIMETHYLPHENYL)THIOSEMICARBAZONES(2012) Gulea, Aurelian; Lozan-Tîrșu, Carolina; Țapcov, Victor; Corja, Ion; Rudic, Valeriu2-Formylpyridine 4-(2,6-dimethylphenyl)-(HL1), 4-(2,5-dimethylphenyl)-(HL2), 4-(3,4-dimethylphenyl)-(HL 3), and 4-(2,4-dimethylphenyl)thiosemicarbazones (HL4) react with copper chloride and nitrate to form coordination compounds CuL 1-4X·nH2O [X = Cl-, NO3 -; n = 1, 2]. All compounds have a polynuclear structure. Azomethines HL1-4 act as the bridging monodeprotonated tridentate N,N,S-ligands. The thermolysis of the complexes includes the dehydration (70-90 C) and total thermal decomposition (350-520 C). The complexes synthesized exhibit a selective antimicrobial activity against a series of standard strains of Staphylococcus aureus and Escherichia coli in the concentration range of 0.009-37.5 μg ml-1Item COPPER(II) COORDINATION COMPOUNDS WITH 2-ACETYLPYRIDINE N4-(BICYCLO[2.2.1]HEPTAN-2-YL)THIOSEMICARBAZONE AS POTENTIAL ANTIBACTERIAL AGENTS(CEP USM, 2023) Graur, Vasilii; Graur, Ianina; Gulea, Aurelian; Teleucă, Iulia; Lozan-Tîrșu, Carolina; Bălan, GretaThe paper presents the synthesis of the new 2-acetylpyridine N4-(bicyclo[2.2.1]hept-2-yl)thiosemicarbazone (HL) and its three copper(II) coordination compounds: [Cu(L)X] (X = NO3- (I), Cl- (II), CHCl2COO- (III)). The obtained compounds were studied by NMR and FTIR spectroscopies, elemental analysis, and molar electric conductibility. The antibacterial activity towards Gram-positive (Staphylococcus aureus, Bacillus cereus) and Gram-negative (Escherichia coli, Acinetobacter baumannii) standard strains was studied for the HL and complexes I-III. The coordination of the HL to the copper(II) atom leads to the increase of activity against almost all microorganisms. Complex I is the most active one towards Gram-positive microorganisms, while complex III is the most active one towards Gram-negative microorganisms. They in many cases surpass the activity of Furacillinum and are practically on the same level as Tetracycline towards Gram-positive microorganisms.Item INHIBITORII PROLIFERĂRII BACTERIEI BACILLUS CEREUS ÎN BAZA COMPUŞILOR COORDINATIVI AI CUPRULUI(II) CARE CONŢIN 4-FENILTIOSEMICARBAZONA 2-FORMILPIRIDINEI ŞI SULFANILAMIDE(2014) Rudic, Valeriu; Lozan-Tîrșu, Carolina; Zariciuc, Elena; Gulea, Aurelian; Țapcov, VictorStudiul dat se referă la obţinerea unui grup de compuşi coordinativi noi de cupru (II) care conţin 4-feniltiosemicarbazona 2-formilpiridinei şi sulfanilamide şi care manifestă activitate antibacteriană pronunţată faţă de bacteriile din genul Bacillus cereus. Proprietăţile stabilite ale compuşilor nominalizaţi asupra altor tipuri de bacterii gram-pozitive şi gramnegative prezintă oportunitate de utilizare în practica medicală din punctul de vedere al extinderii arsenalului de remedii antimicrobiene, iar complecşii respectivi pot fi utilizaţi şi în cazul altor tulpini de microorganisme rezistente la medicamentele tradiţionale.Item NOVEL COPPER(II) COMPLEXES WITH N4,S-DIALLYLISOTHIOSEMICARBAZONES AS POTENTIAL ANTIBACTERIAL/ANTICANCER DRUGS(2023) Graur, Vasilii; Usataia, Irina; Graur, Ianina; Garbuz, Olga; Bouroș, Paulina; Cravțov, Victor; Lozan-Tîrșu, Carolina; Balan, Greta; Fala, Valeriu; Gulea, AurelianThe six new copper(II) coordination compounds [Cu(HL1)Cl2] (1), [Cu(HL1)Br2] (2), [Cu(H2O)(L1)(CH3COO)]·1.75H2O (3), [Cu(HL2)Cl2] (4), [Cu(HL2)Br2] (5), [Cu(H2O)(L2)(CH3COO)] (6) were synthesized with 2-formyl- and 2-acetylpyridine N4,S-diallylisothiosemicarbazones (HL1 and HL2). The new isothiosemicarbazones were characterized by NMR, FTIR spectroscopy, and X-ray crystallography ([H2L2]I). All copper(II) coordination compounds were characterized by elemental analysis, FTIR spectroscopy, and molar conductivity of their 1mM methanol solutions. Furthermore, the crystal structure of complex 3 was determined using single-crystal X-ray diffraction analysis. The studied complexes manifest antibacterial and antifungal activities, that in many cases are close to the activity of medical drugs used in this area, and in some cases even exceed them. The complexes 4 and 5 showed the highest indexes of selectivity (280 and 154) and high antiproliferative activity against BxPC-3 cell lines that surpass the activity of Doxorubicin. The complexes 1–3 also manifest antioxidant activities against cation radicals ABTS•+ that are close to that of trolox, the antioxidant agent used in medicine.Item SYNTHESIS, STRUCTURE, AND ANTIMICROBIAL ACTIVITY OF COPPER(II) CHELATES CONTAINING IMIDAZOLE AND CONDENSATION PRODUCTS OF α-AMINO ACIDS WITH SALICYLALDEHYDE AND ITS DERIVATIVES(2013) Gulea, Aurelian; Lozan-Tîrșu, Carolina; Țapcov, Victor; Ciumacov, Iurie; Janno, E.; Rudic, ValeriuSalicylaldehyde, 5-bromo- and 5-nitrosalicylaldehydes, 2- hydroxynaphthalene-1-carbaldehyde, and 2,3-, 2,4-, and 2,5- dihydroxybenzaldehydes reacted with glycine, alanine, and phenylalanine in ethanol in the presence of imidazole (Im) and copper(II) acetate hydrate to give copper(II) chelates with the composition Cu(Im)(L) · nH2O (H2L is the condensation product of the above aldehydes with α-amino acids; n = 0-2). The structure of the complex Cu(Im)(L 1) [H2L1 = 2-(2-hydroxybenzylideneamino)acetic acid] was determined by X-ray analysis. The crystalline structure of [2-(2-hydroxybenzylideneamino)acetato](imidazole)copper is formed by polymeric chains of the Cu(Im)(L1) molecules linked through bridging oxygen atoms in the carboxy groups of the Schiff base ligand. The coordination unit has a distorted tetragonal pyramid configuration, where the pyramid base is composed of the phenol and carboxy oxygen atoms, CH=N nitrogen atom in the ligand H2L1 and imidazole nitrogen atom. The oxygen atom in the carboxy group in the neighboring molecule occupies the apical position of the coordination pyramid. The other coordination compounds also have polynuclear structure with the Schiff base H2L acting as doubly deprotonated tridentate O,N,O-ligand and bridging carboxy groups. Thermal decomposition of the complexes includes their dehydration (70-95 C), while complete thermal decomposition occurs at 360-530 C. The synthesized complexes showed selective antimicrobial activity in the concentration range from 75 to 300 μg/ml against a number of standard strains of Staphylococcus aureus and Escherichia coli.