ETD system

Electronic theses and dissertations repository

 

Tesi etd-09112017-110518


Thesis type
Tesi di laurea magistrale LM5
Author
BONONI, GIULIA
URN
etd-09112017-110518
Title
Synthesis and biological evaluation of benzoylpiperidine derivatives as MAGL inhibitors
Struttura
FARMACIA
Corso di studi
CHIMICA E TECNOLOGIA FARMACEUTICHE
Commissione
relatore Prof. Minutolo, Filippo
relatore Dott.ssa Granchi, Carlotta
Parole chiave
  • MAGL reversible inhibitors
  • MAGL
Data inizio appello
04/10/2017;
Consultabilità
parziale
Data di rilascio
04/10/2020
Riassunto analitico
Monoacylglycerol lipase (MAGL) is a cytosolic serine hydrolase that plays a major role in the degradation of 2-arachidonoylglycerol, an endocannabinoid neurotransmitter implicated in many physiological and pathological processes, such as pain, inflammation, neuroprotection and cancer. MAGL is upregulated in aggressive cancer cells and primary tumors, where it has a unique role of providing a lipolytic source of free fatty acids for the synthesis of oncogenic signalling lipids, which promote cancer aggressiveness. Recent studies have suggested the possible use of MAGL inhibitors as anti-inflammatory, anti-nociceptive and anti-cancer agents. However, the administration of irreversible MAGL inhibitors may determine an unwanted chronic MAGL inactivation, which causes physical dependence, impairs endocannabinoid-dependent synaptic plasticity and desensitises brain CB1 receptors. Therefore, the aim of my thesis is the synthesis of reversible MAGL inhibitors.
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