Efectul antibacterian şi antifungic al unor compuşi noi

Studiul dat se referă la un grup de substanţe organice noi, care au o activitate pronunţată faţă de bacteriile gram-pozitive, gram-negative, fungi, precum şi toxicitate joasă, şi prezintă o direcţie nouă în elaborarea preparatelor antibacteriene şi antifungice noi

Antimicrobial and antifungal activity of Cu(II) and Bi(III) complexes based on aminopolycarboxylate ions and 2-formyl and 2-acetylpyridine thiosemicarbazones

Moldova State University, Republic of Moldova, Nicolae Testemitanu State University of Medicine and Pharmacy, Republic of MoldovaIntroduction. The biological properties of thiosemicarbazones are often related to metal coordination, which as result affects lipophilicity that controls the rate of entry into the cell. Metal complexes are generally more active than the free ligand, or the metal complex can be a vehicle for activation of the ligand as the cytotoxic agent. Among biologically active metal compounds, copper (II) complexes with 2-formyl and 2-acetylpyridine thiosemicarbazones proved to be among the most potent antiviral, antitumor and anti-inflammatory agents. Bismuth compounds have been widely used in medicine for more than two centuries due to their high effectiveness and low toxicity. In the antimicrobial realm, applications have been widespread, due to bismuth antiseptic, astringent, protective, antacid, antisecretory and local gastrointestinal properties. Material and methods. The research is focused on the synthesis and biological activity investigation of homometallic and heterometallic coordination compounds with 2-formyl (HFopytsc) and 2-acetylpyridine (HAcpytsc) thiosemicarbazones of general formulas {Cu(Fo/Acpytsc)}2Cu(APC)·nH2O, Cu(HFo/Acpytsc)Cu(APC)·nH2O and Bi(HAPC)(HAcpytsc)m·nH2O. Targeting at getting synergistic biological effect, three series of heterometallic coordination compounds of general formula {Cu(Fo/Acpytsc)}Bi(APC)·nH2O with aminopolycarboxylate (APC) ions have been synthesized (n=1- 9; m=1 or 2; APC=ethylenediaminetetraacetate (edta4-), 1,2-cyclohexanediaminetetraacetate (cdta4-) and diethylenetriaminepentaacetate (dtpa5-). The composition and structures of the complexes have been determined by means of elemental analysis, IR spectroscopy and single crystal X-ray diffraction study. Results. The antimicrobial activity of the complexes was evaluated against three bacterial strains, Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Acinetobacter baumannii (BAA-747) Determination of the MIC (minimum inhibitory concentration, mg/mL) and MBC (minimum bactericidal concentration, mg/mL) was carried out by using serial dilutions in liquid broth method. The results demonstrated that Staphylococcus aureus was the most susceptible to the considered compounds. In this case, the values of MIC and MBC vary, ranging from 0.001 to 0.5 mg/mL, indicating high to moderate activity of the compounds. Conclusions. Generally, complexes based on 2-acetylpyridine thiosemicarbazone and edta4- ion, both homo and heterometallic, are more active than the analogues with other APC ligands. The highest antimicrobial activity was displayed by Cu (II) homometallic complex based on 2-acetylpyridine thiosemicarbazone (0.001 mg/mL), followed by its heterometallic Cu (II)-Bi (III) analogue with edta4- ion. Among the complexes with 2- formylpyridine thiosemicarbazone, the derivative of Cu (II) with 4-phenylthiosemicarbazone and edta4- ions displays an activity close to the one displayed by the 2-acetylpyridine representatives

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF COPPER(II), NICKEL(II), COBALT(III) AND IRON(III) COORDINATION COMPOUNDS WITH 2-HYDROXY-3-METHOXYBENZALDEHYDE N(4)-ALLYL-S-METHYLISOTHIOSEMICARBAZONE

The paper presents the synthesis of the 2-hydroxy-3-methoxybenzaldehyde N(4)-allyl-S-methylisothiosemicarba­zone (HL) and seven coordination compounds of copper, nickel, cobalt and iron with this ligand. The new obtained compounds were studied using IR, 1H and 13C NMR spectroscopy, elemental analysis, molar electric conductibility and magnetic susceptibility. The in vitro antiproliferative activity of the HL and synthesized coordination compounds was screened on HeLa cancer cells and normal MDCK cells. The isothiosemicarbazone HL shows better anticancer activity towards HeLa cancer cells than doxorubicin that is used in medical practice and it also practically does not affect the growth and proliferation of normal cells. Moreover, it manifests high antioxidant activity towards ABTS•+ radical cation that exceeds the activity of trolox.</p

Antibacterial efect of some new organic compounds of sulfanilamides range

Laboratorul „Infecţii intraspitaliceşti” USMF „NicolaeTestemiţanu” Catedra chimie anorganică şi fizică USMThis study is refering to a new organic compounds of sulfanilamides range, which shows higher antibacterial activity to grampositive and gramnegative microorganisms and presents a new direction in the elaboration of antibacterial contemporan preparations. Studiul dat se referă la un grup de substanţe sintetice noi din rîndul sulfanilamidelor, care manifestă activitate antibacteriană pronunţată faţă de bacteriile grampozitive şi gramnegative şi, totodată, toxicitate joasă

SINTEZA ȘI STUDIUL PROPRIETĂȚILOR ANTIOXIDATIVE ALE UNOR NOI DERIVAȚI AI BENZOXAZOLILOR

În lucrare este descrisă sinteza a 4 derivați noi ai benzoxazolilor care manifestă proprietăți biologice. A fost stabilită structura compușilor sintetizați cu ajutorul spectroscopiei 1H,13C-RMN, IR, iar pentru N-[2-(dimetilamino)-1,3-benzo­xazol-5-il]-2-[1-(piridin-2-il)etiliden]hidrazin-1-carbotioamidă structura a fost stabilită cu ajutorul difracției cu raze X pe monocristal. Au fost studiate și proprietățile antioxidative ale acestora cu aplicarea metodelor ABTS și DPPH.THE SYNTHESIS AND STUDY OF THE ANTIOXIDATIVE PROPERTIES OF NEW DERIVATIVES OF BENZOXAZOLESIn the present work the synthesis of 4 new derivatives of benzoxazoles with biological properties was carried out. The structure of the synthesized compounds was investigated by the 1H, 13C-NMR, IR spectroscopy and in the case of N-[2-(dimethylamino)-1,3-benzoxazol-5-yl]-2-[1-(pyridin-2-yl)ethylidene]hydrazine-1-carbothioamide by singlecrystal X-ray diffraction determination. The antioxidantive properties were investigated by ABTS and DPPH methods.</p

SYNTHESIS AND BIOLOGICAL ACTIVITY OF COPPER(II), NICKEL(II) AND COBALT(III) COORDINATION COMPOUNDS WITH 2-BENZOYLPYRIDINE N(4)-ALLYL-SMETHYLISOTHIOSEMICARBAZONE

State University of Moldova State University of Medicine and Pharmacy “Nicolae Testemitanu”Lucrarea conţine descrierea sintezei N(4)-alil-S-metilizotiosemicarbazonei 2-benzoilpiridinei (HL) şi a cinci compuşi coordinativi ai cuprului(II), nichelului(II) şi cobaltului(III) cu acest ligand. Compuşii noi obţinuţi au fost studiaţi cu ajutorul spectroscopiei IR şi RMN (1H şi 13C), analizei elementale, conductivitaţii molare şi susceptibilităţii magnetice. Pentru compuşii sintetizaţi a fost determinată in vitro activitatea antibacteriană şi antifungică faţă de spectrul larg de tulpini standard de Staphylococcus aureus (ATCC 25923), Escherihia coli (ATCC 25922), Klebsiella pneumonae şi Candida albicans. Activitatea antiproliferativă in vitro a ligandului şi complecşilor a fost testată pe celule leucemiei mieloide umane HL-60 şi HeLaThis work was fulfilled with the financial support of the Institutional Project 15.817.02.24

Modificările sistemului glutationic eritrocitar în normă şi astm bronşic asociat sub acţiunea unor compuşi biologici activi autohtoni

IP USMF ,,Nicolae Testemițanu”, IMSP Institutul de Ftiziopneumologie „Chiril Draganiuc”, IP Universitatea de Stat a MoldoveiRezumat S-a studiat infl uenţa compuşilor biologic activi (CBA) autohtoni - CMD-4, CMD-8, CMJ-33 şi CMJ-23 asupra indicilor sistemului glutationic eritrocitar (GSH, GR, GPO, GST, G-6-PDH) in vitro în condiţii normale şi în astmul bronşic (AB) de severitate diferită. S-a stabilit că CBA autohtoni exercită efecte modulatoare relevante asupra pricipalelor enzime ale metabolismului GSH, preponderent stimulatoare, fapt ce ar putea fi apreciat ca un răspuns pozitiv ce poate proteja celulele de efectele toxice ale stresului oxidativ specifi c pentru AB. Indicii studiați pot fi folosiți ca biomarcheri informativi pentru monitorizarea procesului patologic și aprecierea efi cienţei preparatelor noi la restabilirea biochimică şi funcţională a sistemelor de protecție celulare în AB și diverse leziuni pulmonare. The modifi cation of erythrocyte glutathione system in normal conditions and asthma, and the infl uence of some local biologically active compounds The infl uence of local biologically active compounds (CBA) - CMD-4, CMD-8, CMJ-33 and CMJ-23 on the indices of erythrocytes glutathione system (GSH, GR, GPO, GST, G-6-PDH) in vitro in normal conditions and asthma (AB) of varying severity was studied. It was established that the local CBA exercises relevant modulatory, mainly stimulants, effects on the key enzymes of the glutathionic metabolism, which could be appreciated as a positive response that can protect cells from the toxic effects of specifi cally for AB oxidative stress. The studied indices can be used as informative biomarkers for monitoring of the pathological process and for assessing of the effectiveness of new compounds for the biochemical and functional restoration of the cellular protection systems in various lung injury. Изменения глутатионовой системы эритроцитов в норме и бронхиальной астме под влиянием некоторых биологически активных соединений Было изучено влияние биологически активных соединений (БAС) - CMD-4, CMD-8, CMJ-33 и CMJ-23 на показатели глутатионовой системы эритроцитов (восстановленный глютатион, глютатион редуктаза, глютатион пероксидаза, глютатион-S-трансфераза, глюкозо-6-фосфат дегидрогеназа) in vitro в норме и при бронхиальной астме (БА) различной степени тяжести. Установлено, что отечественные БАС оказывают модулирующие в основном стимулирующие эффекты на ключевые ферменты метаболизма глутатиона, что можно считать как положительный сдвиг, направленный на защиту клеток от токсического воздействия оксидативного стресса, специфичного для БА. Изученные показатели могут быть использованы в качестве информативных биомаркеров для мониторинга патологического процесса и оценки эффективности новых препаратов для биохимического и функционального восстановления защитных клеточных систем при БА и других легочных заболеваниях

Modificările sistemului glutationic eritrocitar în normă şi astm bronşic asociat sub acţiunea unor compuşi biologici activi autohtoni.

S-a studiat infl uenţa compuşilor biologic activi (CBA) autohtoni - CMD-4, CMD-8, CMJ-33 şi CMJ-23 asupra indicilor sistemului glutationic eritrocitar (GSH, GR, GPO, GST, G-6-PDH) in vitro în condiţii normale şi în astmul bronşic (AB) de severitate diferită. S-a stabilit că CBA autohtoni exercită efecte modulatoare relevante asupra pricipalelor enzime ale metabolismului GSH, preponderent stimulatoare, fapt ce ar putea fi apreciat ca un răspuns pozitiv ce poate proteja celulele de efectele toxice ale stresului oxidativ specifi c pentru AB. Indicii studiați pot fi folosiți ca biomarcheri informativi pentru monitorizarea procesului patologic și aprecierea efi cienţei preparatelor noi la restabilirea biochimică şi funcţională a sistemelor de protecție celulare în AB și diverse leziuni pulmonare

SINTEZA UNOR DERIVAȚI AI 1,2,4-TRIAZOLULUI ÎN BAZA N-[4-(3-METIL-5-SULFANIL-4H-1,2,4-TRIAZOL-4-IL)FENIL]ACETAMIDEI

În articol sunt descrise metodele de sinteză a 8 compuși organici din seria 1,2,4-triazol-3-tiolilor, dintre care 7 compuși sunt noi, a căror structură a fost confirmată prin sinteză și cu ajutorul metodelor spectrale: 1H-RMN, 13C-RMN și IR (FTIR). Compușii (2) și (3) au fost investigați cu ajutorul difracției razelor X pe monocristal. Unii compuși obținuți au demonstrat proprietăți antiproliferative moderate: inhibă creșterea celulelor de HEp-2 și BxPC-3. Activitate antifungică au demonstrat compușii (2) și (7), cu o valoare a CMI de 0,125 μg/mL. Proprietățile antioxidative au fost studiate cu ajutorul metodei ABTS și DPPH; astfel, cel mai bun atioxidant s-a dovedit a fi 2-[(2-hidroxifenil)metiliden]-N-[4-(3-metil-5-sulfanil-4H-1,2,4-triazol-4-il)fenil]hidrazin-1-carbotioamida (7).SYNTHESIS OF DERIVATIVES OF 1,2,4-TRIAZOL BASED ON N-[4-(3-METHYL-5-SULFANYL-4H-1,2,4-TRIAZOL-4-YL)PHENYL]ACETAMIDEThe article describes the synthesis methods of 8 organic compounds from the 1,2,4-triazole-3-thiol series, of which 7 compounds are new. The structure of compounds was confirmed by spectral methods: 1H-NMR, 13C -RMN and IR (FTIR). The triazoles (2) and (3) were investigated by X-ray diffraction on monocrystal. Some compounds have demonstrated moderate antiproliferative properties, in growth of HEp-2 and BxPC-3 cells. Antifungal activity is characteristic far compounds (2) and (7) with a MIC of 0.125 μg/mL. Antioxidative properties were studied using the ABTS and DPPH method where the best one was found to be 2-[(2-hydroxyphenyl)methylidene]-N-[4-(3-methyl-5-sulfanyl-4-triazol-4-yl)phenyl]hydrazine-1-carbothioamide (7).</p