ETD system

Electronic theses and dissertations repository

 

Tesi etd-01312018-083257


Thesis type
Tesi di dottorato di ricerca
Author
GADO, FRANCESCA
URN
etd-01312018-083257
Title
SYNTHESIS AND BIOLOGICAL EVALUATION OF ENDOCANNABINOID SYSTEM MODULATORS
Settore scientifico disciplinare
CHIM/08
Corso di studi
SCIENZA DEL FARMACO E DELLE SOSTANZE BIOATTIVE
Commissione
tutor Prof.ssa Manera, Clementina
commissario Prof.ssa Bertoli, Alessandra
Parole chiave
  • AEA uptake
  • CB1R
  • CB2R
  • endocannabinoid system
  • allosteric modulation
Data inizio appello
05/02/2018;
Consultabilità
parziale
Data di rilascio
05/02/2021
Riassunto analitico
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.<br>Based on the above reported, my PhD thesis can be divided in two main topics:<br>1. Design, synthesis and pharmacological evaluation of new classes of CBRs allosteric modulators:<br>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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