- Synthesis, characterization, crystal structure, electrochemical studies and biological evaluation of metal complexes with thiosemicarbazone of glyoxylic acid
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Cobalt and nickel nitrates form with thiosemicarbazone of glyoxylic acid (H2GAT) complexes of empirical composition Co(C3H4N3O2S)2?2H2O, Ni(C3H4N3O2S)2?2H2O and Ni(C3H6N3O2S)2. X-ray diffraction studies have shown that the Co(HGAT)2?2H2O, Ni(HGAT)2?2H2O complexes are mononuclear, in which the coordination around the metal is octahedral, made up of two sulfur atoms, two nitrogen atoms and two oxygen atoms from two ligands. By the interaction of NiCl2·H2O with 2-[2-(aminothioxomethyl)hydrazinyl] acetic acid (H2TAA) instead of the expected the metal thiosemicarbazonate complex with the hydrogenated on the azomethine group ligand was obtained. The redox properties of these compounds were also investigated by voltammetry on Pt in dimethylsulfoxide/tetrabutylammonium perchlorate. These thiosemicarbazone of glyoxylic acid derivatives had effective inhibition against α-glycosidase, cytosolic carbonic anhydrase I and II isoenzymes, butyrylcholinesterase and acetylcholinesterase. Ki values were found as 26.12–36.58 nM for hCA I, 20.73–40.78 nM for hCA II, 184.30–642.18 nM for AChE, 123.67–342.37 nM for BChE, and 14.66–45.62 nM for α-glycosidase.
- Huseynova, Mansura,Taslimi, Parham,Medjidov, Ajdar,Farzaliyev, Vagif,Aliyeva, Mahizar,Gondolova, Gulnar,?ahin, Onur,Yal??n, Bahattin,Sujayev, Afsun,Orman, Efe Baturhan,?zkaya, Ali R?za,Gul?in, ?lhami
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- Synthesis, biological and theoretical properties of crystal zinc complex with thiosemicarbazone of glyoxylic acid
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A new zinc complex with thiosemicarbazone of glyoxylic acid (1) was synthesized with zinc acetate dihydrate and thiosemicarbazone of glyoxylic acid and crystallized in water. The absolute crystal structure of the complex was defined using the single-crystal X-ray diffraction technique. It was seen in X-ray measurements that the complex crystallized in the triclinic system with the P-1 space group. The structure of 1 represents distorted octahedral geometry around the central zinc metal. Zn(II) complex with thiosemicarbazone of glyoxylic acid was an inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), human carbonic anhydrase I and II isoforms (hCA I and II) receptors and the inhibitor constant (Ki) values of the synthesized complex were 38.94 ± 8.2 μM for hCA I, 48.62 ± 11.3 μM for hCA II, 65.16 ± 11.4 μM for BChE and 82.04 ± 16.0 μM for AChE, respectively. The molecular docking method was used to show the complex-enzyme interactions. The pharmacokinetic properties of the complex were determined by ADME/Tox predictions and the results obtained showed that the complex could be a potential drug candidate.
- Huseynova, Mansura,Farzaliyev, Vaqif,Medjidov, Ajdar,Aliyeva, Mahizar,?zdemir, Mücahit,Taslimi, Parham,Zorlu, Yunus,Yal??n, Bahattin,?ahin, Onur
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- Dimethyl sulfoxide containing platinum(II) and palladium(II) chelate complexes of glyoxylic and pyruvic acid thiosemicarbazones. A new class of cytotoxic metal complexes
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The complexes [Pt(DMSO)(GT)]·DMSO (1), [Pt(DMSO)(PT)]·1/2DMSO (2) and [Pd(DMSO)(PT)] (3), where DMSO = dimethyl sulfoxide, H2GT = glyoxylic acid thiosemicarbazone and H2PT = pyruvic acid thiosemicarbazone, have been synthesized and characterized by elemental analysis, molar electric conductivity, IR, electronic and NMR (1H and 13C) spectra. The single crystal X-ray diffraction analysis has revealed for 1 (orthorhombic, Pnma, a = 12.941(3), b = 7.108(2), c = 15.148(3) A?, Z = 4) that the doubly deprotonated thiosemicarbazone molecule is coordinated to Pt(II) via the carboxylato O, azomethine N and thiolato S atoms forming two condensed five-membered chelate rings. The fourth coordination site of Pt(II) is occupied by the S atom of DMSO. All the atoms of the complex molecule are coplanar except the methyl groups. The O atom of DMSO is in cis-position towards the thiolato-S atom (point group Cs). A system of hydrogen bonds of the type N-H?O links the complex molecules between them and with the lattice DMSO molecules. Similar structures have been deduced for the remaining two complexes on the basis of spectroscopic data. The three complexes and the ligand H2GT exhibit cytotoxic activity against F4N leukemia cells, whereas the ligand H2PT is inactive.
- Dodoff, Nicolay I.,Kovala-Demertzi, Dimitra,Kubiak, Maria,Kuduk-Jaworska, Janina,Kochel, Andrzej,Gorneva, Galina A.
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p. 1110 - 1122
(2008/09/19)
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