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Synthesis, characterization, antibacterial evaluation and molecular docking studies of 2-azetidinone derivatives as novel DNA gyrase inhibitors

Sulthana R. M., Quine S. D.

International Letters of Chemistry, Physics and Astronomy

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2015

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Vol. 47

94--108

EN

Newly designed 2-azetidinone derivatives (4a-e) were synthesized in good yields and characterised by advanced spectroscopic studies. The title compounds were evaluated for qualitative (zone of inhibition) by agar diffusion method against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa and Streptococcus pyogenes. Some of the analogues were found to have comparable or even more potency than the standard drugs. Docking study was performed to check interaction of synthesized compounds with the target DNA gyrase.

2

Synthesis, Structural Investigation and Biological Studies of Some Transition Metal Chelates of Acid Hydrazone

Yaul A. R., Dhande V. V., Suryawanshi N. J., Aswar A. S.

Polish Journal of Chemistry

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2009

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Vol. 83, nr 4

565-571

EN

Metal complexes of Ti(III), VO(IV), Cr(III), Mn(III), Fe(III) and Zr(IV) with Schiff base derived from 2-hydroxy-5-methylacetophenone and benzoyl hydrazide have been synthesized and characterized on the basis of elementalanalysis, infrared spectra, magnetic moment, electronic spectra and thermogravimetric studies. Various kinetic parameters evaluated from thermal decomposition data and thermal stabilities of the complexes are also reported. The antibacterial and antifungal activities of 2-hydroxy- 5-methylacetophenone benzoylhydrazone (HMABH) and its complexes have been investigated against various bacterial strains using the disc diffusion technique. All complexes exhibit good biological activity as compared to free ligand. Solid-state electrical conductivity of ligand and its complexes have also been studied over a wide range of temperature and it was found that compounds exhibit semiconucting behavior in the studied range.

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Synthesis and Characterization of Copper(II) and Synthesis Nickel(II) Complexes of Isonitrosoacetophenone 4-Aminobenzoylhydrazone

Usluer O., Gup R.

Polish Journal of Chemistry

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2007

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Vol. 81, nr 7

1257-1265

EN

Two types of copper complexes as well as an oximate bridged nickel complex with a new tridentate ligand containing a monoxime and hydrazone moieties have been prepared and characterized by elemental analyses, IR, 1H NMR, UV-VIS and magnetic susceptibility measurements. The reaction of isonitrosoacetophenone 4-aminobenzoylhydrazone (H2L) with CuCl2ź2H2O gives the complex [Cu(H2L)Cl2] where the ligand acts as a neutral O,N,N-tridentate and the coordination takes place in the keto form. The acylhydrazoneoxime ligand reacts with copper(II) and nickel(II) acetate in the presence of the strong base to produce common bimetal(II) oximato complex, [{M(L)}2] in which two copper(II) and nickel(II) atoms are bridged through two N-O bridges of the oximato ligand to afford a binuclear structure. The effects of varying pH and solvent on the absorption behavior of both ligand and complexes have been investigated.

4

Cobalt(II), Copper(II), Nickel(II), and Zinc(II) Complexes of Naphthaldehyde Thiazolyl Hydrazones

Yilmaz I., Çukurovali A.

Polish Journal of Chemistry

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2004

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Vol. 78 / nr 5

663-672

EN

Two new Schiff base ligands containing 2,4-disubstituted thiazoles and cyclobutane rings, 2-hydroxy-1-naphthaldehyde [4-(3-methyl-3-mesitylcyclobutyl)-1,3-thiazol- 2-yl] hydrazone (L1H) and 1-(2-hydroxy-1-naphthyl)etanone [4-(3-methyl-3-mesitylcyclobutyl)- 1,3-thiazol-2-yl] hydrazone (L2H) and their mononuclear complexes with a 1:2 metal:ligand ratio have been prepared from chloride salts of Co(II), Cu(II), Ni(II) and Zn(II) in EtOH. The authenticity of new ligands and their complexes have been established by elemental analyses, infrared, 1H and 13CNMRspectra, and by magnetic susceptibility measurements. Thermal properties of the ligands and complexes have been studied by thermogravimetric analysis (TGA) technique. The novel complexes of transition metal ions contain two monoanionic, bidentate NO ligands. It was found that all the complexes are mononuclear.

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Reactions of 3-Hydrazino-1,2,4-triazino[5,6-b]indole with alfa, beta-unsaturated ketones, esters and nitriles

Youssef A. S. A.

Bulletin of the Polish Academy of Sciences. Chemistry

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2001

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Vol. 49, No. 1

9-16

EN

3-Hydrazino-l,2,4-triazino[5,6-b]indole (1) reacted with l-aryl-3-phenylprop- 2-yn-l-ones (Ila-c) to give 3-1'-(5'-aryl-3'-phenyl)pyrazolyl] 1,2,4-triazino[5,6-b]indoles (Illa-c). o;-(p-Chlorobenzoyl) acephenone-N-3(l,2,4-triazino[5,6-b]indole) hydrazone (IV) was isolated in case of (lib) only. On the other hand, methyl p-chlorophenyl prop-2-ynoate (lid) gave 3-[1'-(3'-p-chlorophenyl-5'-hydroxy) pyrazolyl] l,2,4-triazino[5,6-b]indo-le (Hid). (I) reacted with diethyl but-2-yndioate (VI) to give 3-[1'-(3'-carboethoxy-4'-hydro-5'-oxo) pyrazolyl] l,2,4-triazino[5,6-b]indole (VII) and diethyl oxaloacetate- N- 3-(1,2,4-triazino[5,6-b]indole) hydrazone (VIII). Similar treatment of (I) with 2-cyano-(IXa) or 2-cyano-3-methyl- (IXb) cinnamonitriles afforded 3-[2'-(4'-phenylmethylene-3',5'-dioxo-4'-hydro) pyrazolyl] - (Xa) or 3-[2'-(4'-methyl phenylmethylene-3',5'-dioxo-4'-hydro) pyrazolyl]- (Xb) l,2,4-triazino[5,6-b] indoles, respectively.

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N-(E)-2-Stilbenyloxymethylenecarbonyl substituted hydrazones of ortho, meta and para hydroxybenzaldehydes

Wyrzykiewicz E., Błaszczyk A., Turowska-Tyrk I.

Bulletin of the Polish Academy of Sciences. Chemistry

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2000

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Vol. 48, No. 3

213-229

EN

Twelve unknown N-(E)-2-stilbenyloxymethylenecarbonyl substituted hydra-zones of acetone and ortho, meta and para hydroxybenzaldehydes have been prepared. The N-substituted hydrazones occur as E geometrical isomers and cis/trans amide conformers (1) H NMR estimations). Crystal structures of N-(E)-2-stilbenyloxymethylenecarbonyl sub-stituted hydrazone of ortho hydroxy-benzaldehyde 10 and N-(E)-2/-(4/-chlorostilbenyloxy-methylenecarbonyl)-substituted hydrazone of meta hydroxybenzaldehyde 14 have been determined as E geometrical isomers and trans amide conformers with intra- (10) and intermolecular (14) hydrogen bonds.