RESUMEN
In the present paper, a novel series of dibenzofuran-piperazine derivatives were synthesized via the treatment of N-(2-methoxy-3-dibenzofuranyl)-2-chloroacetamide with substituted piperazine derivatives. The chemical structures of the compounds were elucidated by (1)H NMR, (13)C NMR, mass spectral data; elemental analysis and HPLC analysis. Each derivative was evaluated for antiplatelet activity and anticholinesterase activity. Compound 2 m with 2-furoyl moiety exhibited high percentage inhibition as much as standard drug aspirin on arachidonic acid (AA)-induced platelet aggregation. None of the compounds presented significant inhibitor effect on collagen-induced platelet aggregation. Furthermore, the anticholinesterase activity of the compounds was determined and they did not show promising inhibitor activity compared with standard drug donepezil.
Asunto(s)
Benzofuranos/química , Piperazinas/síntesis química , Piperazinas/farmacología , Piperazina , Piperazinas/química , Inhibidores de Agregación Plaquetaria/farmacologíaRESUMEN
In this study, 14 different 2-[(1-methyl-1H-tetrazole-5-yl)thio]-1-(phenyl)ethanone derivatives (1-14) were synthesized. The structures of the obtained compounds were elucidated using IR, (1)H-NMR, (13)C-NMR and FAB(+)-MS spectral data and elemental analyses results. The compounds were screened for their anticandidal activity using the microbroth dilution method and for their cytotoxic effects using the MTT assay against NIH/3T3 cells. Some of the compounds were found to be potent anticandidal agents with weak cytotoxicities.
Asunto(s)
Candida/efectos de los fármacos , Tetrazoles/síntesis química , Tetrazoles/farmacología , Animales , Espectroscopía de Resonancia Magnética , Ratones , Pruebas de Sensibilidad Microbiana , Células 3T3 NIH , Espectrometría de Masa Bombardeada por Átomos VelocesRESUMEN
In this study, nine new hydrazide derivatives were synthesized. The reaction of 2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide with various benzaldehydes or acetophenones resulted in N'-substituted-2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide derivatives. The structure elucidation of the synthesized and purified compounds was performed by using IR, (1)H-NMR, and FAB(+)-MS spectral data and elemental analyses, respectively. Furthermore, the compounds were screened and evaluated for their antifungal activity against a panel of different human pathogenic Candida strains such as C. albicans, C. glabrata, C. utilis, C. tropicalis, C. krusei, C. zeylanoides and C. parapsilosis using agar diffusion and broth microdilution assays, respectively. Some of the tested compounds showed comparable antifungal activity (MIC = 0.0156->2 mg/mL) with ketoconazole.
Asunto(s)
Antifúngicos/síntesis química , Antifúngicos/farmacología , Candida/efectos de los fármacos , Hidrazinas/farmacología , Naftalenos/farmacología , Antifúngicos/química , Relación Dosis-Respuesta a Droga , Hidrazinas/síntesis química , Hidrazinas/química , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Naftalenos/síntesis química , Naftalenos/química , Relación Estructura-ActividadRESUMEN
PURPOSE: A number of neurological disorders are marked by increased or aberrant frequency of neuronal discharge in specific parts of the brain. Administration of drugs such as antiepileptic compounds results in the depression of neuronal activity in the whole brain, with the potential for serious side-effects. In the search for additional therapies to reduce the unphysiological electrical activity of over-active brain foci, we have examined the effect of fibroblasts transplanted to areas responsible for motor dysfunction in hemi-parkinsonian rats, since bursting synchronous discharges in internal segment of globus pallidus (GPi) are thought to be partially responsible for the movement disorders of PD. Fibroblasts express gap junctions and ion channels, and so, when transplanted to brain tissue, can potentially modulate excessive electrical activity. METHODS: Neonatal cortical neurons were cultured on multi-electrode arrays, and their electrical activity was evaluated before and after fibroblast seeding. Unilateral 6-hydroxydopamine (6-OHDA) lesion was carried out in Fischer rats. Lesioned or control rats were transplanted with either syngeneic dermal fibroblasts, microfine glass beads, ibotenic acid, or physiological saline, in the entopeduncular nucleus (EP). Apomorphine-induced rotational behavior and L-dopa-induced dyskinetic movements were evaluated before transplantation (baseline) and 2, 4, 8, 12, and 24 weeks following transplantation. Following behavioral experiments, rats were perfused with 4% formaldehyde in PBS for immunohistochemical study of the brain. RESULTS: We demonstrate in vitro that the introduction of fibroblasts into a network of neurons does not interfere with overall functional measures of activity, while moderately altering the characteristics of synchronous neuronal discharge. In rats with unilateral 6-hydroxydopamine lesions of the nigro-striatal dopaminergic pathway, apomorphine-induced rotations were reduced by more than 60% following ipsilateral transplantation of fibroblasts to the EP. L-Dopa-induced dyskinesia was also significantly reduced. Transplantation of inert microspheres, or chemical lesion of the same area with ibotenic acid, did not produce beneficial effects on parkinsonian symptomatology. CONCLUSION: Fibroblast transplantation could be an alternative treatment strategy for the parkinsonian patient.
Asunto(s)
Discinesia Inducida por Medicamentos/terapia , Fibroblastos/trasplante , Actividad Motora/fisiología , Neuronas/fisiología , Enfermedad de Parkinson Secundaria/terapia , Animales , Discinesia Inducida por Medicamentos/fisiopatología , Oxidopamina , Enfermedad de Parkinson Secundaria/inducido químicamente , Enfermedad de Parkinson Secundaria/fisiopatología , Ratas , Ratas Endogámicas F344 , Ratas Sprague-Dawley , Resultado del TratamientoRESUMEN
In this study, some 1-methylene-2,3-diaryl-1,2-dihydropyrazino[1,2-a]benzimidazole and some 1-(2-arylvinyl)-3-arylpyrazino[1,2-a]benzimidazole derivatives were synthesised. The structure elucidation of the compounds was performed by IR, 1H-NMR and MASS spectroscopic data and elemental analyses results. Anticancer and anti-HIV activities of the compounds were examined, however no anti-HIV activity was seen; highly notable anticancer activity was obtained. It was also observed that the compounds were more potent against leukaemia cell lines.