RESUMEN
Three fluoro-barbiturates were synthesised, showing in vivo sedative efficacy. One of them, [(18)F], was synthesised in radiofluorinated form. PET/CT Imaging with [(18)F] identified ß-amyloid over-expressing transgenic mice (ßA mice) compared to wild type and tau lines. The fluorescent barbiturate 9 was able to label ßA plaques in brain sections of ßA mice, and co-localise with a fluorescent Zn(II) indicator.
Asunto(s)
Enfermedad de Alzheimer/diagnóstico por imagen , Péptidos beta-Amiloides/análisis , Barbitúricos , Encéfalo/diagnóstico por imagen , Radioisótopos de Flúor , Placa Amiloide/diagnóstico por imagen , Enfermedad de Alzheimer/diagnóstico , Enfermedad de Alzheimer/genética , Péptidos beta-Amiloides/genética , Animales , Barbitúricos/química , Encéfalo/metabolismo , Radioisótopos de Flúor/química , Humanos , Ratones , Ratones Endogámicos C57BL , Ratones Transgénicos , Placa Amiloide/genética , Tomografía de Emisión de Positrones/métodos , Regulación hacia Arriba , Proteínas tau/análisisRESUMEN
1-(2-Pyridyl)-2-propen-1-ol, obtained by vinylation of commercially available picolinaldehyde, resulted a good starting material for the synthesis of the indolizidine skeleton. In particular, a simple process involving bromination, reduction, and nucleophilic substitution (via elimination and addition) allowed an easy conversion of the starting material into (±)-lentiginosine in ~27% overall yield.
