RESUMEN

Lycorane is a pentacyclic core presented in alkaloids isolated from the Amaryllidaceae family of herbaceous flowering plants. Members of this class of natural products have shown to display important biological properties including analgesic, antiviral, and antiproliferative activities. This review presents the known synthetic routes toward α-, ß-, γ-, and δ-lycoranes. α-(19 routes), ß-(10 routes), γ-(38 routes), and δ-(6 routes).

RESUMEN

We have developed versatile methods toward the synthesis of a variety of piperidine/piperazine bridged isosteres of pridopidine. The compounds were assessed against the D2 receptor in agonist and antagonist modes and against the D4 receptor in agonist mode. hERG Binding and the ADME profiles were studied.

Asunto(s)

Diseño de Fármacos , Piperazina/química , Piperidinas/química , Animales , Compuestos Bicíclicos con Puentes/síntesis química , Compuestos Bicíclicos con Puentes/química , Compuestos Bicíclicos con Puentes/farmacología , Cristalografía por Rayos X , Antagonistas de Dopamina/síntesis química , Antagonistas de Dopamina/química , Antagonistas de Dopamina/farmacología , Canal de Potasio ERG1/metabolismo , Humanos , Espectroscopía de Resonancia Magnética , Ratones , Piperazina/síntesis química , Piperazina/farmacología , Piperidinas/síntesis química , Piperidinas/farmacología , Receptores de Dopamina D2/agonistas , Receptores de Dopamina D4/agonistas , Receptores de Dopamina D4/antagonistas & inhibidores , Relación Estructura-Actividad