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1.
Eur J Med Chem ; 42(3): 394-402, 2007 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-17224205

RESUMEN

A few (1:1) and (1:2) metal complexes of cobalt(II), nickel(II), copper(II) and zinc(II) have been isolated with ligand derived from the condensation of 4-amino-3-mercapto-6-methyl-5-oxo-1,2,4-triazine with 2-acetylpyridine (L(1)) and characterized by elemental analysis, conductivity measurements, infrared, electronic, (1)H NMR spectral data, magnetic and thermogravimetric analyses. Due to insolubility in water and most of the common organic solvents and infusibility at higher temperatures, all the complexes are thought to be polymeric in nature. A square-planar geometry was suggested for copper(II) and octahedral proposed for cobalt(II), nickel(II) and zinc(II). Some of the chemically synthesized compounds have been screened in vitro against the three Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis and Bacillus subtilis) and two Gram-negative (Salmonella typhi and Escherichia coli) organisms. It is observed that the coordination of metal ion has pronounced effect on the microbial activities of the ligand. The metal complexes have higher antimicrobial effect than the free ligands.


Asunto(s)
Antibacterianos/síntesis química , Antibacterianos/farmacología , Metales/química , Bases de Schiff/síntesis química , Compuestos de Sulfhidrilo/síntesis química , Compuestos de Sulfhidrilo/farmacología , Triazinas/síntesis química , Triazinas/farmacología , Fenómenos Químicos , Química Física , Cobalto/química , Cobre/química , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Indicadores y Reactivos , Ligandos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Níquel/química , Espectrofotometría Infrarroja , Termogravimetría , Zinc/química
2.
J Enzyme Inhib Med Chem ; 21(5): 557-62, 2006 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-17194027

RESUMEN

Antibacterial Schiff bases derived from 1,2,4-triazoles as well as their metal complexes incorporating cobalt(II), nickel(II), copper(II) and zinc(II) have been synthesized and characterized. Physico-chemical studies suggest that an octahedral geometry for the cobalt(II), nickel(II) and zinc(II)and square-planer geometry for the copper(II) complexes. These complexes have been screened for antibacterial activity against three Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis and Bacillus subtilis) and two Gram-negative (Salmonella typhi and Pseudomonas aeruginosa) bacterial strains, and results compared with the activity of the free ligands. The metal complexes were found to be more potent against one or more bacterial strains than the free ligands.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Benzaldehídos/química , Benzaldehídos/farmacología , Metales Pesados/farmacología , Triazoles/química , Triazoles/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Metales Pesados/química , Estructura Molecular , Bases de Schiff/química , Análisis Espectral , Relación Estructura-Actividad , Temperatura
3.
Eur J Med Chem ; 41(1): 147-53, 2006 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-16271421

RESUMEN

A series of metal complexes of Co(II), Ni(II), Cu(II) and Zn(II) have been synthesized with newly prepared biologically active ligands. These ligands were prepared by the condensation of 4-amino-5-mercapto-3-methyl-s-triazole (AMMT), 4-Amino-3-ethyl-5-mercapto-s-triazole (AEMT) with 2-acetylpyridine. The structure of the complexes have been proposed by elemental analyses, spectroscopic data i.e. IR, 1H NMR, electronic and magnetic measurements. Thermal studies of the complexes are also reported. Antibacterial activities of 10 complexes have been studied in vitro. Heterocyclic bidentate Schiff bases were associated with substantially higher antibacterial activities than some commercial antibiotics.


Asunto(s)
Cobalto , Cobre , Cetonas/química , Níquel , Bases de Schiff/química , Triazoles , Compuestos de Zinc , Antibacterianos/química , Antibacterianos/metabolismo , Cobalto/química , Cobalto/metabolismo , Cobre/química , Cobre/metabolismo , Bacterias Gramnegativas/efectos de los fármacos , Ligandos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Níquel/química , Níquel/metabolismo , Espectrofotometría Infrarroja , Triazoles/síntesis química , Triazoles/metabolismo , Compuestos de Zinc/síntesis química , Compuestos de Zinc/metabolismo
4.
J Enzyme Inhib Med Chem ; 21(6): 749-55, 2006 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-17252949

RESUMEN

Schiff bases have been synthesized by the reaction of p-nitrobenzaldehyde, o-nitrobenzaldehyde and p-toluyaldehyde with 4-amino-5-mercapto-1,2,4-triazole. The ligands react with Co(II), Ni(II) and Zn(II) metals to yield (1:1) and (1:2) [metal:ligand] complexes. Elemental analyses, IR, 1H NMR, electronic spectral data, magnetic susceptibility measurements, molar conductivity measurements and thermal studies have investigated the structure of the ligands and their metal complexes. The electronic spectral data suggests octahedral geometry for Co(II), Ni(II) and Zn(II). The antibacterial activities of the ligands and their metal complexes have been screened in vitro against three Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis and Bacillus subtilis) and two Gram-negative (Salmonella typhi and Pseudomonas aeruginosa) organisms. The coordination of the metal ion had a pronounced effect on the microbial activities of the ligands and the metal complexes have higher antimicrobial effect than the free ligands.


Asunto(s)
Antibacterianos/química , Antibacterianos/farmacología , Metales Pesados/química , Metales Pesados/farmacología , Nitrógeno/química , Azufre/química , Ligandos , Bases de Schiff/síntesis química , Bases de Schiff/química
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