RESUMEN
Several N-substituted-N'-[4-(4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thione -5-yl ) phenyl[thioureas were synthesized in order to examine their antibacterial and antifungal activities. The structures and purity of the synthesized compounds were confirmed by UV, IR and mass spectral data and elemental analysis. However, they were found not to possess significant antibacterial or antifungal activity.
Asunto(s)
Antiinfecciosos/síntesis química , Antifúngicos/síntesis química , Tiazoles/síntesis química , Tiourea/análogos & derivados , Antibacterianos , Antiinfecciosos/farmacología , Antifúngicos/farmacología , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta , Tiazoles/farmacología , Tiourea/síntesis química , Tiourea/farmacologíaRESUMEN
3-Methyl-4-[(2,4-dihydro-4-substituted-3H-1,2,4-triazole-3-thione-5-yl) phenylhydrazono]-5-isoxazolone derivatives have been synthesised. The structure of these compounds was determined using spectral data and elemental analyses. These compounds were tested for antimicrobial activity.
Asunto(s)
Antiinfecciosos/síntesis química , Antifúngicos/síntesis química , Isoxazoles/síntesis química , Tiazoles/síntesis química , Antibacterianos , Antiinfecciosos/química , Antiinfecciosos/farmacología , Antifúngicos/química , Antifúngicos/farmacología , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Isoxazoles/química , Isoxazoles/farmacología , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta , Tiazoles/química , Tiazoles/farmacologíaRESUMEN
A new series of 4-substituted benzylideneamino-5[3(5)-methyl-5(3)-phenyl-1H-1-pyrazolyl]-2 ,4-dihydro-3H- 1,2,4-triazole-3-thione was synthesized by reaction of I with suitable aldehyde and tested for their antimicrobial activities against six microorganisms. Most of the compounds showed antibacterial activity against Gram positive bacteria.
Asunto(s)
Antiinfecciosos/síntesis química , Compuestos de Bencilideno/síntesis química , Pirazoles/síntesis química , Tionas/síntesis química , Triazoles/síntesis química , Antibacterianos , Antiinfecciosos/farmacología , Compuestos de Bencilideno/farmacología , Fenómenos Químicos , Química Física , Hongos/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Pirazoles/farmacología , Relación Estructura-Actividad , Tionas/farmacología , Triazoles/farmacologíaRESUMEN
Benzoic acid p-amino-[(substituted phenyl/pyridyl) methylene] hydrazide derivatives were synthesised by interaction of p-aminobenzoic acid hydrazide with various aromatic aldehydes. The structures of the compounds were elucidated by use of their UV, IR, 1H-NMR and mass spectral data. These compounds were also evaluated for antimicrobial activity. The in vitro hepatic microsomal metabolism of benzoic acid p-amino-[(4-fluorophenyl)methylene]hydrazide (2d), a selected prototype from these compounds was also carried out.
Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Hidrazonas/síntesis química , Hidrazonas/farmacología , Microsomas Hepáticos/metabolismo , Animales , Antibacterianos , Antiinfecciosos/metabolismo , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Hidrazonas/metabolismo , Técnicas In Vitro , Masculino , Pruebas de Sensibilidad Microbiana , RatasAsunto(s)
Infección Hospitalaria/epidemiología , Infecciones del Sistema Respiratorio/epidemiología , Anciano , Ampicilina/uso terapéutico , Anticuerpos Antibacterianos/análisis , Anticuerpos Antivirales/análisis , Combinación de Medicamentos/uso terapéutico , Femenino , Departamentos de Hospitales , Humanos , Cuidados a Largo Plazo , Masculino , Persona de Mediana Edad , Ápice del Flujo Espiratorio , Estudios Prospectivos , Distribución Aleatoria , Infecciones del Sistema Respiratorio/diagnóstico , Infecciones del Sistema Respiratorio/tratamiento farmacológico , Sulfametoxazol/uso terapéutico , Trimetoprim/uso terapéutico , Combinación Trimetoprim y SulfametoxazolRESUMEN
In order to investigate the effect of kefir consumption on mucositis induced by 5-FU based chemotherapy (CT), we monitored the systemic immune response by measurement of the serum proinflammatory cytokine levels and we evaluated the anti-microbial effect of kefir with an agar diffusion method. Forty patients with colorectal cancer were included in this randomized prospective study. On the first 5 days of each CT cycle, the study group received oral lavage with kefir and then swallowed 250 ml of kefir while control group received oral lavage with 0.09% NaCl twice a day. Before and after every cycle of CT, the oral mucosa was assessed. Serum proinflammatory cytokine levels were evaluated before the initiation and after the third and the sixth cycle. Kefir was administered in 99 out of 205 courses. Mucositis developed in 27.3% of the courses given with kefir administration and in 21.7% of the courses given with 0.9% NaCl oral rinses. The difference between the two groups was not statistically significant (p > 0.05). When we compared the serum proinflammatory cytokine levels of the two groups at the baseline and following the third and the sixth cycles, we again found no statistically significant difference (p > 0.05). Kefir consumption at the mentioned doses made no statistically significant effect on serum proinflammatory cytokine levels and on the incidence of mucositis development in cancer patients. Under in vitro conditions, kefir inhibits only Staphylococcus epidermidis.
Asunto(s)
Antimetabolitos Antineoplásicos/efectos adversos , Productos Lácteos Cultivados , Fluorouracilo/efectos adversos , Estomatitis/prevención & control , Administración Oral , Adulto , Anciano , Neoplasias Colorrectales/tratamiento farmacológico , Citocinas/sangre , Citocinas/efectos de los fármacos , Femenino , Humanos , Mediadores de Inflamación/sangre , Masculino , Persona de Mediana Edad , Mucosa Bucal/efectos de los fármacos , Mucosa Bucal/patología , Estudios Prospectivos , Estomatitis/inducido químicamente , Adulto JovenRESUMEN
OBJECTIVES: This study was carried out prospectively to determine the effect on prognosis of phagocytic activity index (PAI) and intracellular killing activity (IKA) of polymorphonuclear leukocytes (PMNL), and the levels of interleukin-1 beta (IL-1beta) on prognosis in patients with diabetic foot infection (DFI). METHODS: The evaluation of PAI and IKA in PMNL and the levels of IL-1beta were performed at the beginning and in the second and fourth weeks of therapy in all diabetic patients, who were categorized into a healing group (HG) and a non-healing group (NHG) on the basis of therapy results. RESULTS: Sixty-six cases (38 diabetic patients and 28 non-diabetic controls) were included in the study. Full recovery was observed in 23 HG patients, whereas 15 (NHG) patients were unresponsive to treatment and nine patients were subjected to amputation at the end. At the baseline, PAI, IKA and IL-1beta levels in HG were not significantly different compared to those of NHG, but at weeks 2 and 4, PAI and IKA levels were significantly higher and IL-1beta levels were significantly lower than those in NHG. On the other hand, at the baseline, PAI and IKA values in HG were significantly lower and IL-1beta levels were significantly higher in comparison with the controls. However, no significant difference was observed at week 2 or 4. CONCLUSION: Our results suggest that the PMNL functions and IL-1beta regulation deteriorated in patients with DFI, and that such deteriorations might indicate inefficient therapeutic responses in patients with diabetes mellitus.
Asunto(s)
Pie Diabético/inmunología , Pruebas Inmunológicas , Interleucina-1beta/inmunología , Neutrófilos/inmunología , Cicatrización de Heridas/inmunología , Adulto , Anciano , Anciano de 80 o más Años , Femenino , Humanos , Interleucina-1beta/sangre , Masculino , Persona de Mediana Edad , Fagocitosis , Pronóstico , Estudios ProspectivosRESUMEN
Levels of Streptococcus mutans in plaque samples from margins of conventional and high copper amalgam restorations were compared in fourteen patients, each having one conventional amalgam filling in each quadrant and one high copper amalgam filling on the contra-lateral side were examined. The percentage of S. mutans of total CFU count in plaque was higher on conventional amalgam than on high copper amalgam. The difference was statistically significant (p < 0.01).
Asunto(s)
Cobre/farmacología , Amalgama Dental/química , Placa Dental/microbiología , Streptococcus mutans/efectos de los fármacos , Adolescente , Adulto , Recuento de Colonia Microbiana , Humanos , Streptococcus mutans/aislamiento & purificaciónRESUMEN
The in vitro effect of amikacin (8 microg/ml), imipenem (30 microg/ml), cefodizime (10 microg/ml), interferon alpha-2a (IFNalpha-2a) (10 IU/ml) and antibiotic combinations with IFNalpha-2a on polymorphonuclear leukocyte (PMN) functions (phagocytosis and intracellular killing of Candida albicans blastospores) was investigated in chronic hepatitis B patients. Phagocytosis and candidacidal activity was not affected after pretreatment of PMNs with amikacin and imipenem (p > 0.05). Phagocytic activity was enhanced after pretreatment of PMNs with cefodizime and IFNalpha-2a compared with that of control PMNs (p < 0.05), but candidacidal activity was not affected by the same drugs (p > 0.05). Phagocytic and intracellular activity of PMNs were not affected by combinations of IFNalpha-2a and antibiotics (p > 0.05).
Asunto(s)
Antiinfecciosos/farmacología , Cefotaxima/análogos & derivados , Cefotaxima/farmacología , Hepatitis B Crónica/tratamiento farmacológico , Imipenem/farmacología , Interferón-alfa/farmacología , Neutrófilos/efectos de los fármacos , Adulto , Amicacina/farmacología , Análisis de Varianza , Quimioterapia Combinada , Humanos , Interferón alfa-2 , Fagocitosis/efectos de los fármacos , Proteínas RecombinantesRESUMEN
BACKGROUND: It has been shown that antibacterial agents affect polymorphonuclear leukocytes (PMNs), which are active in the body's first line of defense, in different ways. However, few studies have investigated the effects of tablet dosage forms as opposed to pure powder forms. There is a need to demonstrate the clinical relevance of previous results with commercially available products. METHODS: We examined the effects of clarithromycin solutions, prepared separately from either pure powder or commercially available tablets (250 mg), on human PMNs. The in vitro effects of each solution, adjusted to therapeutic concentration (1 mg/l), on PMN adherence, chemotaxis, phagocytosis, candidacidal capacity and superoxide production were studied. RESULTS: Solutions prepared from pure clarithromycin powder did not affect the adherence, phagocytosis or superoxide production of PMNs, but did inhibit (p<0.05) chemotaxis and candidacidal capacity. By contrast, a decrease (p<0.05) in all functions except phagocytosis was observed with solutions prepared from the tablet dosage form of clarithromycin. CONCLUSION: The results of this study suggest that the tablet dosage form of clarithromycin may have a more pronounced inhibitory effect on human PMN functions than solutions prepared from the pure powder form.
Asunto(s)
Antibacterianos/farmacología , Claritromicina/farmacología , Neutrófilos/efectos de los fármacos , Neutrófilos/fisiología , Adhesión Celular/efectos de los fármacos , Quimiotaxis/efectos de los fármacos , Claritromicina/administración & dosificación , Composición de Medicamentos , Humanos , Fagocitosis/efectos de los fármacos , Superóxidos/metabolismo , ComprimidosRESUMEN
Polymorphonuclear leucocytes (PMNs) are important components of host defence against fungi. We investigated the ex vivo effect of fluconazole on chemotaxis, adherence, superoxide anion (O-2) generation and intracellular killing of Candida albicans blastoconidia after the administration of fluconazole (300 mg per os) to healthy volunteers. With regard to chemotaxis in response to zymosan-activated serum (ZAS), as measured using an agarose gel technique, fluconazole neither increased, nor decreased the chemotaxis of PMNs. The adherence was significantly enhanced after exposure of PMNs to fluconazole under ex vivo conditions, whereas, O-2 production after stimulation of PMNs with ZAS was not affected by fluconazole. The effect of fluconazole on intracellular killing of C. albicans blastoconidia by PMNs was determined by viable colony count, after release of yeast cells from disturbed neutrophils. Fluconazole under in vitro conditions, at a therapeutic concentration, significantly increased the intracellular killing of C. albicans by PMNs at 30 min when compared with the results obtained in ex vivo experiments (p < 0.001). During 90 min of exposure, no significant difference was found between in vitro and ex vivo conditions (p > 0.05).