Data di Pubblicazione:
2005
Citazione:
New Muscle Relaxant Glycosylthiocolchicine derivatives / G. Pontremoli ; Tutor: Maria Luisa GELMI; Coordinatore: Carlo DE MICHELI. DIPARTIMENTO DI SCIENZE MOLECOLARI APPLICATE AI BIOSISTEMI, 2005. 18. ciclo, Anno Accademico 2004/2005.
Abstract:
A novel class of 3-demethoxy-3-glycosylaminothiocolchicines (7) was prepared and tested for muscle relaxant
activity. The syntheses were performed starting from the new 3-amino-3-demethoxythiocolchicine (5) prepared
in good yield from 3-O-demethylthiocolchicine (1c) using the Buchwald-Hartwig reaction. The condensation
of 5 with a series of pentose and hexose sugars (6) gave a series of 3-demethoxy-3-glycosylaminothiocolchicines
(7). Their preparation was accomplished by adapting and improving a previous procedure for
the preparation of N-arylglycosylamines. In particular, replacing traditional heating with microwave irradiation
represents the key improvement of the process. The biological activity of the 3-demethoxy-3-glycosylaminothiocolchicines
(7) was evaluated on GABA and strychnine-sensitive glycine receptors present in rat
brain and spinal cord.
Tipologia IRIS:
13 - Tesi di dottorato discussa entro ottobre 2010
Elenco autori:
G. Pontremoli
Link alla scheda completa: