RESUMEN
Herein, we describe a simple and general multi-component synthesis of 5-arylselanyluracils by the regioselective C-H selenation of uracils. Reactions of uracils with arylboronic acid and Se powder in the presence of AgNO3 (10 mol%) at 120 °C under aerobic conditions afforded various 5-arylselanyluracils. The source of the introduced selanyl group was prepared from a commercially available arylboronic acid and Se powder in the reaction system, thereby ensuring a simple and efficient protocol. This reaction represents the first example of the synthesis of a 5-arylselanyluracil in a multi-component system.
RESUMEN
We studied the effect of fluoroquinolones (FQs) on carrageenan-induced edema in the rat footpad. Ciprofloxacin, gatifloxacin, sparfloxacin, norfloxacin, and enoxacin (s.c., 100 mg/kg), which have piperazinyl and/or cyclopropyl groups, inhibited carrageenan-induced edema, whereas levofloxacin, tosufloxacin, and pazufloxacin did not. The reduction of edema by ciprofloxacin, sparfloxacin, and enoxacin was abolished by pretreatment with mifepristone, an antagonist of the glucocorticoid receptor. These results suggest that FQs with piperazinyl and/or cyclopropyl groups can modify biological responses through enhancing the glucocorticoid-glucocorticoid receptor system.
Asunto(s)
Edema/tratamiento farmacológico , Edema/metabolismo , Fluoroquinolonas/farmacología , Receptores de Glucocorticoides/metabolismo , Análisis de Varianza , Animales , Carragenina , Relación Dosis-Respuesta a Droga , Edema/inducido químicamente , Fluoroquinolonas/administración & dosificación , Pie , Masculino , Mifepristona/farmacología , Ratas , Ratas Wistar , Relación Estructura-ActividadRESUMEN
The area distribution of out-issued prescriptions for outpatients in Saiseikai Kurihashi Hospital was surveyed over 6 months from the first day of out-issue. Behavior patterns of outpatients in the selection of pharmacy were also investigated. Our survey included the out-issued prescriptions in eight surrounding newly established pharmacies together with the first out-issue. Computer simulation indicated that 70% of the outpatients selected the surrounding pharmacies when they received their out-issued prescriptions the first time. However, the percentage of surrounding pharmacies selected by the patients decreased to 60% the second time, and then again increased to 80% the third time. The results suggest that most outpatients use surrounding pharmacies, although they try to use the pharmacies near their homes for a time.
