RESUMEN
BACKGROUND: Dual-source CT allows scanning of the chest with high pitch and high temporal resolution, which can improve the detection of proximal coronary arteries in infants and young children when scanned without general anesthesia, sedation or beta-blockade. OBJECTIVE: To compare coronary artery visibility between higher and standard temporal resolution. MATERIALS AND METHODS: We analyzed CT images in 93 children who underwent a standard chest CT angiographic examination with reconstruction of images with a temporal resolution of 75 ms (group 1) and 140 ms (group 2). RESULTS: The percentage of detected coronary segments was higher in group 1 than in group 2 when considering all segments (group 1: 27%; group 2: 24%; P = 0.0004) and proximal segments (group 1: 37%; group 2: 32%; P = 0.0006). In both groups, the highest rates of detection were observed for the left main coronary artery (S1) (group 1: 65%; group 2: 58%) and proximal left anterior descending coronary artery (S2) (group 1: 43%; group 2: 42%). Higher rates of detection were seen in group 1 for the left main coronary artery (P = 0.03), proximal right coronary artery (P = 0.01), proximal segments of the left coronary artery (P = 0.02) and proximal segments of the left and right coronary arteries (P = 0.0006). CONCLUSION: Higher temporal resolution improved the visibility of proximal coronary arteries in pediatric chest CT.
Asunto(s)
Angiografía Coronaria/métodos , Procesamiento de Imagen Asistido por Computador/métodos , Tomografía Computarizada por Rayos X/métodos , Preescolar , Femenino , Humanos , Lactante , Masculino , Reproducibilidad de los Resultados , RespiraciónRESUMEN
CONTEXT: Inhibition of pathological angiogenesis. OBJECTIVE: Obtaining new transactivator, bifunctional, thyroid antagonist, non-toxic anti-angiogenic compounds. MATERIALS AND METHODS: In silico drug design, synthesis in bulk and biological evaluation in chick chorioallantoic membrane (CAM) model. RESULTS: Significant inhibition (range 65-73%) at 0.25-2.0 µg/ml doses. DISCUSSION AND CONCLUSION: The synthesis of compounds (9), (10), and (11) incorporating long-chain moieties guanidine, urea, methyl amine and, propyl amine substitutions, respectively, into the core molecular framework of tetrac (tetraiodothyroacetic acid) were undertaken. The evaluation of the anti-angiogenic bioactivity of these compounds in the CAM model revealed no loss of activity in comparison with tetrac and XT199, which showed nearly 86% inhibition at dose levels of 1 and 0.5 µg/ml, respectively, and validated the concept.
Asunto(s)
Inhibidores de la Angiogénesis/farmacología , Diseño de Fármacos , Integrina alfaVbeta3/antagonistas & inhibidores , Glándula Tiroides/efectos de los fármacos , Inhibidores de la Angiogénesis/síntesis química , Inhibidores de la Angiogénesis/química , Animales , Pollos , Relación Dosis-Respuesta a Droga , Huevos , Modelos Moleculares , Estructura MolecularRESUMEN
Research on dual inhibitors of both 5-LOX and COXs gained interest due to the overexpressions of these enzymes during the malignant state of the evolution of prostate cancer. In order to take part in this research, new N-aroyl-tetrahydro-gamma-carbolines issued from the modification of Indomethacin have been synthesised. As for the NSAIDs, the compounds have been tested for their activity against COX(1), COX(2) plus against 5-LOX and against the proliferation of malignant prostate cancer. Interesting cytotoxic activities and selectivities of some tetrahydro-gamma-carboline derivatives have been obtained.
Asunto(s)
Carbolinas/síntesis química , Inhibidores de la Ciclooxigenasa/síntesis química , Inhibidores de la Lipooxigenasa , Neoplasias de la Próstata/tratamiento farmacológico , Antiinflamatorios no Esteroideos/farmacología , Carbolinas/farmacología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Inhibidores de la Ciclooxigenasa/farmacología , Humanos , Indometacina , Masculino , Relación Estructura-ActividadRESUMEN
Novel thyroxine analogs with hindered phenol, amino and carboxylic acid groups have been synthesized and the effects of the synthesized compounds on angiogenesis using the chick chorioallantoic membrane and mouse matrigel models have been tested. Pharmacological profiles revealed that thyroxine tolerates numerous modifications on the amino group and remains active. These results provide the rationale for the selection of a novel thyroxine nanoparticle precursor.
Asunto(s)
Inhibidores de la Angiogénesis/síntesis química , Inhibidores de la Angiogénesis/farmacología , Tiroxina/síntesis química , Tiroxina/farmacología , Animales , Embrión de Pollo , Ratones , Modelos Moleculares , Tiroxina/análogos & derivadosRESUMEN
Novel Tetrac analogs were synthesized and then tested. Anti-angiogenesis efficacy was carried out using the Chick Chorioallantoic Membrane (CAM) model and the mouse matrigel model for angiogenesis. Pharmacological activities showed Tetrac can accommodate numerous modifications and maintain anti-angiogenesis activity.
Asunto(s)
Inhibidores de la Angiogénesis/química , Tiroxina/análogos & derivados , Inhibidores de la Angiogénesis/farmacología , Animales , Embrión de Pollo , Membrana Corioalantoides/irrigación sanguínea , Membrana Corioalantoides/efectos de los fármacos , Evaluación Preclínica de Medicamentos , Factores de Crecimiento de Fibroblastos/farmacología , Hemoglobinas/análisis , Ratones , Relación Estructura-Actividad , Tiroxina/síntesis química , Tiroxina/química , Tiroxina/farmacologíaRESUMEN
A series of new 9-substituted acridyl derivatives were synthesized and their in vitro antimalarial activity was evaluated against one chloroquine-sensitive strain (3D7) and three chloroquine-resistant strains [W2 (Indochina), Bre1 (Brazil) and FCR3 (Gambia)] of Plasmodium falciparum. Some compounds inhibit the growth of malarial parasite with IC50 Asunto(s)
Acridinas/farmacología
, Antimaláricos/farmacología
, Plasmodium falciparum/efectos de los fármacos
, Acridinas/síntesis química
, Acridinas/química
, Animales
, Antimaláricos/síntesis química
, Antimaláricos/química
, Estructura Molecular
, Pruebas de Sensibilidad Parasitaria
, Plasmodium falciparum/crecimiento & desarrollo
, Estereoisomerismo
, Relación Estructura-Actividad