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1.
Bioorg Chem ; 106: 104494, 2021 01.
Artigo em Inglês | MEDLINE | ID: mdl-33268009

RESUMO

1,2-diborolanes with strong and without strong donor substituents have been described, and are also referred to as 1,2-diboracyclopentane. The 1,2-diaryl/alkyl-amino-1,2-diboracyclopentanes 2, 3, and 4 were obtained in good yield after the reaction of 1,2-dichloro-1,2-diboracyclopentane 1 with ArNHLi and Me3Si-NR2. The structures of these new derivatives were characterized by nuclear magnetic resonance spectroscopy. The molecular structures of 2b, 2c, 2e, 4, and 5f were also determined by single-crystal X-ray diffraction. The newly synthesized 1,2-borolanes are stable in air and showed particularly high activity against some Gram-positive bacteria.


Assuntos
Antibacterianos/farmacologia , Compostos de Boro/farmacologia , Bactérias Gram-Positivas/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/química , Compostos de Boro/síntese química , Compostos de Boro/química , Relação Dose-Resposta a Droga , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
2.
Braz. J. Pharm. Sci. (Online) ; 53(1): e15075, 2017. tab, graf
Artigo em Inglês | LILACS | ID: biblio-839452

RESUMO

ABSTRACT Unsymmetrically substituted imidazolium salts were synthesized and characterized using 1H-NMR and 13C-NMR. The antimicrobial activities of the salts were evaluated using the agar-well diffusion method against 14 bacteria and five yeasts. The minimal inhibitory concentrations (MIC) against seven bacteria and one yeast were also determined. Among the test compounds applied, 1, 2, 3, 6 and 11 showed activities against Micrococcus luteus ATCC 9341, Staphylococcus aureus ATCC 25923, Staphylococcus epidermidis ATCC 12228, Bacilllus cereus ATCC 11778, Bacillus subtilis ATCC 6633, Bacillus thuringiensis, Listeria monocytogenes ATCC 19112 and Candida trophicalis. However, compounds 1, 2 and 3 showed the highest antimicrobial activities against Micrococcus luteus ATCC 9341, Stapylococcus aureus ATCC 25923, Staphylococcus epidermidis ATCC 12228, Bacilllus cereus ATCC 11778 and Bacillus subtilis ATCC 6633 with inhibition zones of 14-20 mm. In addition, compound 6 have only demonstrated activities against Candida trophicalis while compounds 4, 5, 7, 8, 9, 10, 12, 13 and 14 had no effect on test microorganisms.


Assuntos
Sais/análise , Imidazóis/farmacocinética , Anti-Infecciosos/análise , Espectroscopia de Ressonância Magnética/instrumentação , Imidazóis/metabolismo
3.
Bioinorg Chem Appl ; 2014: 718175, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25332694

RESUMO

Reaction of 1-phenyl-3-methyl-4-benzoyl-pyrazol-5-one and benzoyl hydrazide in refluxing ethanol gave N (')-[(Z)-(3-methyl-5-oxo-1-phenyl-1,5-dihydro-4H-pyrazol-4-ylidene)(phenyl)methyl]benzohydrazide (HL(1)), which was characterized by NMR spectroscopy and single-crystal X-ray structure study. X-ray diffraction analyses of the crystals revealed a nonplanar molecule, existing in the keto-amine form, with intermolecular hydrogen bonding forming a seven-membered ring system. The reaction of HL(1) with Co(II), Ni(II), and Cu(II) halides gave the corresponding complexes, which were characterized by elemental analysis, molar conductance, magnetic measurements, and infrared and electronic spectral studies. The compounds were screened for their in vitro cytotoxic activity against HL-60 human promyelocytic leukemia cells and antimicrobial activity against some bacteria and yeasts. Results showed that the compounds are potent against HL-60 cells with the IC50 value ≤5 µM, while some of the compounds were active against few studied Gram-positive bacteria.

4.
Artigo em Inglês | MEDLINE | ID: mdl-24239764

RESUMO

Two novel vicinal dioxime ligands containing (4-methoxybenzaldehyde thiosemicarbazone glyoxime (L(1)H2) or 4-ethoxybenzaldehyde thiosemicarbazone glyoxime (L(2)H2)) thiosemicarbazone units were synthesized and characterized using (1)H NMR, (13)C NMR, HMQC, MS, infrared and, UV-VIS. spectroscopy, elemental analysis, and magnetic susceptibility measurements. Mononuclear nickel(II), copper(II) and cobalt(II) complexes with a metal:ligand ratio of 1:2 for L(1)H2 and L(2)H2 were also synthesized. The effect of pH and solvent on the absorption spectra of both ligands and complexes was determined. IR spectra show that the ligands act in a bidentate manner and coordinates N4 donor groups of the ligands to Ni(II), Cu(II) and Co(II) ions. The detection of H-bonding (O-H⋯O) in the [M(LH)2] metal complexes by IR spectra supported the square-planar MN4 coordination of mononuclear complexes. The antimicrobial activities of compounds L(1)H2, L(2)H2, and their Ni(II), Cu(II) and Co(II) complexes were evaluated using the disc diffusion method against 12 bacteria and 4 yeasts. The minimal inhibitory concentrations (MICs) against 7 bacteria and 3 yeasts were also determined. Among the test compounds attempted, L(1)H2, [Ni(L1H)2], [Cu(L1H)2], L2H2, [Ni(L2H)2] and [Cu(L2H)2] showed some activities against certain Gram-positive bacteria and some of the yeasts tested.


Assuntos
Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , Metais Pesados/farmacologia , Oximas/química , Oximas/farmacologia , Tiossemicarbazonas/química , Tiossemicarbazonas/farmacologia , Absorção , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Cobalto/farmacologia , Complexos de Coordenação/síntese química , Cobre/farmacologia , Elétrons , Fungos/efeitos dos fármacos , Concentração de Íons de Hidrogênio , Ligantes , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Conformação Molecular , Níquel/farmacologia , Oximas/síntese química , Solventes/química , Espectrofotometria Infravermelho , Espectrofotometria Ultravioleta , Tiossemicarbazonas/síntese química
5.
Appl Biochem Biotechnol ; 171(8): 2285-94, 2013 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-24068477

RESUMO

In this work, bacterial cellulose nanofibers were produced by using the Gluconacetobacter hansenii HE1 strain. These nanofibers were derivatized with dye affinity ligand Reactive Green 5, and these newly synthesized dye-attached nanofibers were used for affinity adsorption of urease. Reactive Green 5-attached nanofibers were characterized by Fourier transform infrared spectroscopy, SEM, and energy-dispersive x-ray spectroscopy analysis. Some adsorption conditions which significantly affect the adsorption efficiency were investigated. The maximum urease adsorption capacity was found to be 240 mg/g nanofiber in pH 6.0 and at room temperature. Dye-free plain nanofibers also used for studying nonspecific urease adsorption onto plain nanofibers and nonspecific adsorption were found to be negligible (3.5 mg/g nanofiber). Prepared dye-attached nanofibers can be used in five successive adsorption/desorption steps without any decrease in their urease adsorption capacity. The desorption rate of the adsorbed urease was found to be 98.9 %. The activity of the urease was also investigated, and it was found that free and desorbed urease from the dye-attached nanofibers showed similar specific activity.


Assuntos
Adsorção , Gluconacetobacter/química , Nanofibras/química , Urease/química , Celulose/química , Corantes/química , Enzimas Imobilizadas/química , Espectroscopia de Infravermelho com Transformada de Fourier
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