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1.
J Inorg Biochem ; 141: 58-69, 2014 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-25217718

RESUMEN

The synthesis and microbiological evaluation of two new Ag(I) complexes with sulfamoxole (SMX), [Ag2(SMX)2]·H2O and [Ag4(SCN)3(SMX)]·H2O are described. Both were characterized by elemental analysis, thermogravimetry, powder and single crystal X-ray diffraction, NMR, Raman and experimental and theoretical IR spectroscopies. Their antibacterial and antifungal properties were evaluated by agar and broth dilution assays, respectively. In addition, synergism tests for Pseudomonas aeruginosa were performed, and genotoxicity studies were carried out employing the Allium cepa test. Both complexes displayed good activity against Escherichia coli, Staphylococcus aureus, P. aeruginosa, and 10 fungi strains, with lower minimum inhibitory concentrations (MICs) than that of free SMX in all cases. The nanometrical crystallite particle size determined from XRPD, DLS and TEM might explain the good microbiological activity in spite of the low solubility of both complexes. The fractional inhibitory concentration (FIC) calculated from the P. aeruginosa test data indicated that the activity of the complexes is not due to synergism of the free components in the concentration ratios studied. Moreover, none of the complexes displayed cytotoxic effects on onions in the concentration range tested, and chromosome aberrations were not observed.


Asunto(s)
Antibacterianos/síntesis química , Antifúngicos/síntesis química , Complejos de Coordinación/síntesis química , Sulfamoxol/síntesis química , Antibacterianos/farmacología , Antifúngicos/farmacología , Complejos de Coordinación/farmacología , Cristalografía por Rayos X , Hongos/efectos de los fármacos , Hongos/crecimiento & desarrollo , Pruebas de Sensibilidad Microbiana , Pruebas de Mutagenicidad , Nanopartículas/química , Nanopartículas/ultraestructura , Cebollas/citología , Cebollas/efectos de los fármacos , Cebollas/crecimiento & desarrollo , Tamaño de la Partícula , Pseudomonas aeruginosa/efectos de los fármacos , Pseudomonas aeruginosa/crecimiento & desarrollo , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/crecimiento & desarrollo , Sulfamoxol/farmacología
2.
ChemMedChem ; 9(6): 1211-20, 2014 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-24806993

RESUMEN

We report the synthesis, characterization, antibacterial and antifungal activities, phytotoxicity, and genotoxicity of two new complexes of silver(I) with sulfachloropyridazine (SCP), one of which is heteroleptic with SCP and SCN(-) ligands (Ag-SCP-SCN), the other of which is homoleptic (Ag-SCP); furthermore, the crystal structure of the homoleptic complex is disclosed. The heterocyclic N atom nearest to the Cl atom and the N(sulfonamide) atom could be coordination sites for the silver ion in the Ag-SCP-SCN complex. The Ag-SCP complex is a polymeric compound with metal-metal bonds, and the heterocyclic and sulfonamide N atoms are points of coordination for Ag(I) . Both complexes showed activity against all the tested bacteria, and in the cases of Escherichia coli and Pseudomonas aeruginosa, the action was better than that of SCP. In all cases, both silver-SCP complexes showed better antifungal activity than SCP, which was inactive against the tested fungi. Notably, the activity against P. aeruginosa, a nosocomial multidrug-resistant pathogen, was better than that of the reference antibiotic cefotaxim. Both silver-sulfa complexes displayed moderate activity against the tested yeast, especially for C. neoformans, which is an important fact considering the incidence of cryptococcosis, mainly in immune-deficient patients. No chromosomal aberrations were observed with the Allium cepa test, which is auspicious for further study of these complexes as potential drugs.


Asunto(s)
Antibacterianos/química , Antifúngicos/química , Complejos de Coordinación/química , Plata/química , Sulfaclorpiridazina/análogos & derivados , Allium/genética , Antibacterianos/síntesis química , Antibacterianos/toxicidad , Antifúngicos/síntesis química , Antifúngicos/toxicidad , Candida/efectos de los fármacos , Aberraciones Cromosómicas/efectos de los fármacos , Complejos de Coordinación/síntesis química , Complejos de Coordinación/toxicidad , Cristalografía por Rayos X , Escherichia coli/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Conformación Molecular , Pruebas de Mutagenicidad , Pseudomonas aeruginosa/efectos de los fármacos , Sulfaclorpiridazina/síntesis química , Sulfaclorpiridazina/química , Sulfaclorpiridazina/toxicidad , Tiocianatos/química
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