5351-23-5Relevant articles and documents
Synthesis, characterization and antioxidant activity of new dibasic tridentate ligands: X-ray crystal structures of DMSO adducts of 1,3-dimethyl-5-acetyl-barbituric acid o-hydroxybenzoyl hydrazone copper(II) complex
Giziroglu, Emrah,Aygün, Muhittin,Sarikurkcu, Cengiz,Kazar, Didem,Orhan, Nil,Firinci, Erkan,Soyleyici, H. Can,Gokcen, Ceren
, p. 199 - 205 (2013)
o-Hydroxybenzoyl hydrazine and p-hydroxybenzoyl hydrazine react with 1,3-dimethyl-5-acetyl-barbituric acid in ethanol to give H2L 1 (85% yield) and H2L2 (91% yield) respectively. The copper(II) complexes with DMSO adducts, [Cu(L 1)(DMSO)] and [Cu(L2)(DMSO)], were prepared by the stoichiometric reaction of the CuCl2·5H2O with the H2L1 and H2L2 in a molar ratio (M:L) of 1:1 in DMSO/water mixture. All compounds have been fully characterized using conventional spectroscopic techniques. X-ray structure analysis was carried out on the [Cu(L1)(DMSO)] which crystallizes in the triclinic P-1 space group. In addition, both ligands were applied several antioxidant assays including total antioxidant activity by phosphomolybdate, ferric reducing antioxidant power (FRAP) and scavenging activity on 1,1-diphenyl-2- picrylhydrazyl (DPPH). The results from antioxidant assays have shown that both ligands have excellent activities.
Seven coordinated cobalt(II) complexes with 2,6-diacetylpyridine bis(4-acylhydrazone) ligands: Synthesis, characterization, DNA-binding and nuclease activity
G?k?e, Cansu,Dilek, Nefise,Gup, Ramazan
, p. 213 - 220 (2015)
A new series of pentadentate 2,6-diacetylpyridine bis(4-acylhydrazone)s (H2L1 and H2L2) based seven-coordinated cobalt(II) complexes, [Co(Ln)X2] (n = 1 and X = DMF for (1); n = 2 and X = H2O for (2)); [Co(H2Ln)Y2] (n = 1 or 2; Y = N3- or NCS-), has been synthesized and characterized by using spectroscopic techniques. Single crystal X-ray study of [Co(L1)(DMF)2] (1) complex exhibits pentagonal-bipyramidal coordination geometry where the pentadentate N3O2 ligand in the equatorial plane of the bipyramid and two dimethylformamide molecules in the axial area. Interaction of the cobalt(II) complexes with CT DNA has been investigated by absorption titration method and viscosity measurements which reveal that the cobalt(II) complexes could bind with CT DNA through intercalation. Cleavage activity of the complexes (1) and (2) with pBR 322 plasmid DNA was evaluated by agarose gel electrophoresis demonstrating that the ability of the complexes to cleave the pBR 322 plasmid DNA via oxidative pathway, possibly due to the involvement of a diffusible hydroxyl radical mechanism in presence and absence of an oxidative agent. The nuclease activity of the Co(II) complexes has strong dependence on the concentration of complex and reaction time, both in presence and absence of hydrogen peroxide.
Seven-coordinated cobalt(II) complexes with 2,6-diacetylpyridine bis(4-hydroxybenzoylhydrazone): Synthesis, characterisation, DNA binding and cleavage properties
Gup, Ramazan,G?k?e, Cansu,Dilek, Nefise
, p. 629 - 641 (2015)
Synthesis and characterisation of three seven-coordinated cobalt(II) complexes of 2,6-diacetylpyridine bis(4-hydroxybenzoylhydrazone) (H4L) ligand, [Co(H2L)(H2O)2] (1), [Co(H4L)(N3)2] (2) and [Co(H4L)(NCS)2] (3) are described. The structures of the complexes were characterised by elemental analysis, IR, UV-vis and magnetic susceptibility measurement. The molecular structure of the [Co(H4L)(NCS)2] (3) was also determined by X-ray crystallography. Single crystal X-ray revealed that the Co(II) complex (3) has a pentagonal-bipyramidal coordination geometry, with pentadentate N3O2 ligand in the equatorial plane of the bipyramid and two isothiocyanato groups in the axial area. Interaction of the cobalt(II) complexes with CT-DNA was investigated by absorption titration method and viscosity measurements. Cleavage activity of the complexes with pBR 322 plasmid DNA was evaluated by agarose gel electrophoresis in presence and absence of an oxidative agent, and the mechanism of DNA cleavage was investigated. The results suggest that the cobalt(II) complexes bind effectively and they exhibit nuclease activity, which has strong dependence on the concentration of complex and reaction time, both in presence and absence of hydrogen peroxide.
Pleuromutilin derivative with 1, 3, 4-oxadiazole side chain and preparation and application thereof
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Paragraph 0055-0056; 0070; 0090; 0093; 0095; 0103, (2021/07/24)
The invention belongs to the field of medicinal chemistry, and particularly relates to a pleuromutilin derivative with a 1, 3, 4-oxadiazole side chain and preparation and application thereof The pleuromutilin derivative with the 1, 3, 4-oxadiazole side chain is a compound shown in a formula 2 or a pharmaceutically acceptable salt thereof, and a solvent compound, an enantiomer, a diastereoisomer and a tautomer of the compound shown in the formula 2 or the pharmaceutically acceptable salt thereof or a mixture of the solvent compound, the enantiomer, the diastereoisomer and the tautomer in any proportion, including a racemic mixture. The pleuromutilin derivative has good antibacterial activity, is especially suitable for being used as a novel antibacterial agent for systemic system infection of animals or human beings, and has good water solubility.
Molecular docking studies, biological evaluation and synthesis of novel 3-mercapto-1,2,4-triazole derivatives
Ghanaat, Javad,Khalilzadeh, Mohammad A.,Zareyee, Daryoush
, p. 223 - 232 (2020/02/25)
Abstract: Synthesis of bioactive heterocyclic compounds having effective biological activity is an essential research area for wide-ranging applications. In this study, a conventional methodology has been developed for the synthesis of a series of new 3-mercapto-1,2,4-triazole derivatives 4a–f. The purity and structure of the synthesized molecules were confirmed by 1H NMR, 13C NMR and elemental analysis. In addition, the prepared compounds were screened for their anti-proliferative activity against three human cancer cell lines including A549 (lung cancer), MCF7 (breast cancer) and SKOV3 (ovarian cancer) using MTT reduction assay. All the tested compounds demonstrated remarkable cytotoxic activity with IC50 values ranging from 3.02 to 15.37?μM. The heterocyclic compound bearing 3,4,5-trimethoxy moiety was found to be the most effective among the series displaying an IC50 of 3.02?μM specifically against the ovarian carcinoma cancer cell line (SKOV3). Moreover, Annexin V-FITC/propidium iodide staining assay indicated that this compound can induce apoptosis in SKOV3 cells. Furthermore, cell cycle assay showed a significant cell cycle arrest at the G2/M phase in a dose-dependent manner for this compound. The molecular docking results was showed binding modes of potent compound 4d perfectly corroborated the suggestion of binding to the colchicine site. The entire results conclude that 3-mercapto-1,2,4-triazole derivatives can be synthesized by a green method for biological and pharmacological applications. Graphic abstract: New analogs of 3-mercapto-1,2,4-triazole potential derivatives for anti-proliferative activity were synthesized. Cytotoxic activity of all synthesized compounds was evaluated against tree human cancer cell lines: lung (A549), breast (MCF7) and ovarian (SKOV3).[Figure not available: see fulltext.].
