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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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.
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