ETD

Archivio digitale delle tesi discusse presso l'Università di Pisa

Tesi etd-01312018-083257


Tipo di tesi
Tesi di dottorato di ricerca
Autore
GADO, FRANCESCA
URN
etd-01312018-083257
Titolo
SYNTHESIS AND BIOLOGICAL EVALUATION OF ENDOCANNABINOID SYSTEM MODULATORS
Settore scientifico disciplinare
CHIM/08
Corso di studi
SCIENZA DEL FARMACO E DELLE SOSTANZE BIOATTIVE
Relatori
tutor Prof.ssa Manera, Clementina
commissario Prof.ssa Bertoli, Alessandra
Parole chiave
  • endocannabinoid system
  • CB2R
  • CB1R
  • allosteric modulation
  • AEA uptake
Data inizio appello
05/02/2018
Consultabilità
Completa
Riassunto
The endocannabinoid system (ECS) is a ubiquitous neuromodulator system with wide-ranging actions, consisting on cannabinoid receptors (CB1R and CB2R), their endogenous ligands (endocannabinoids, EC) and the enzymes for EC synthesis and degradation. Since the discovery of allosteric binding site(s) on the CBRs, medicinal chem- istry research has been focusing on the development of different classes of allosteric modulators as they might offer a novel therapeutic approach with minimized side-effects. Moreover, EC degradation and membrane transporter inhibitors have been developed as they constitute an alternative therapeutic ap- proach to raise the levels of the EC preserving the beneficial effects derived from the direct activation of CBRs.
Based on the above reported, my PhD thesis can be divided in two main topics:
1. Design, synthesis and pharmacological evaluation of new classes of CBRs allosteric modulators:
2. Design, synthesis and pharmacological evaluation of 2-oxo-1,2-dihydro- pyridine-3-carboxamide derivatives as EC degradation and membrane transporter inhibitors.
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