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Nuovi principi attivi e relative formulazioni per la terapia del dolore ed il trattamento dei tumori

Lazzari, Paolo (2014) Nuovi principi attivi e relative formulazioni per la terapia del dolore ed il trattamento dei tumori. Doctoral Thesis.

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Abstract

The discovery of novel drugs for chronic pain treatment, as well as for chemotherapy, characterized by significant efficacy and reduced side effects is one of the main goals of the medicinal chemistry.
In this work, novel pyrazole cannabinoid ligands and diazabicycloalkyl delta opioid derivatives have been synthetized and their pharmacological profiles have been investigated to evaluate their potential application in chronic/inflammatory or neuropathic pain therapies. According to the determined pharmacological profiles, lead compounds belong to the investigated series may represent useful candidates for the treatment of these pathologies.
In addition, a novel fluorinated thiol endopeptidase inhibitor has been investigated as alternative strategy to manage inflammatory pain. The compound showed interesting pharmacological profile in formalin test by evidencing higher activity and improved bioavailability compared to reference inhibitors.
Considering the sparingly solubility of cannabinoidergic and opioidergic compounds, part of the work has been devoted to the obtainment and the characterization of injectable aqueous formulations of these agents based on microemulsion systems.
Novel tubulysin derivatives as innovative agents for chemotherapy have been synthetized through an improved process. The novel tubulysins evidenced high cytotoxicity towards various cancer cell lines and significant activity in an animal model of resistant tumor to conventional chemotherapic agents.

Item Type:Doctoral Thesis
ID Code:9551
Contributors:Pinna, Gérard Aimé
Publisher:Università degli studi di Sassari
Uncontrolled Keywords:Pain, cannabinoid, opioid, chemotherapy, tubulysins
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Cicli, scuole e corsi:Ciclo 26 > Scienze e Tecnologie chimiche > Scienze farmaceutiche
Deposited On:01 Apr 2014 09:42

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