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Digital archive of theses discussed at the University of Pisa

 

Thesis etd-05072020-231429


Thesis type
Tesi di laurea magistrale LM5
Author
MOSCATELLI, SERENA
URN
etd-05072020-231429
Thesis title
Investigation of an unprecedented backbone functionalization method for the obtainment of novel imidazole containing derivatives
Department
FARMACIA
Course of study
CHIMICA E TECNOLOGIA FARMACEUTICHE
Supervisors
relatore Prof.ssa La Motta, Concettina
relatore Prof. Bjørsvik, Hans-René
Keywords
  • synthetic optimization of imidazole-based compound
  • spinal muscular atrophy
Graduation session start date
27/05/2020
Availability
Withheld
Release date
27/05/2090
Summary
The experimental work of my master thesis has been carried out at the Department of Chemistry of the University of Bergen (NO), under the supervision of Professor Hans-René Bjørsvik and within the framework of the Erasmusprogramme.
The work has been focused on the synthesis of the novel derivative, 3-chloro-4-fluoro-N-(5-(1-hydroxycyclobutyl)-1-methyl-1H-imidazol-4-yl)benzamide, characterized by the presence of an imidazole residue and designed by suitably modifying similar compounds already developed in the Bjørsvik’s lab for the treatment ofSpinal Muscular Atrophy (SMA).
In particular, the molecular scaffold of the previously obtained compounds has been modified through the insertion of an imidazole residue, in order to get to novel active analogues.
Insertion of an imidazole nucleus is an important synthetic strategy in drug discovery. Actually, this heterocycle represents an integral part of alkaloids and is present in a series of other compounds with great diversity in biological activity, which includes cytotoxic, antifungal,and antibacterial properties.
The relevant therapeutic properties of imidazole-related drugs have always pushed medicinal chemists to synthesize and test a large number of novel molecules bearing this heterocyclic residue, which has now become a privileged scaffold in medicinal chemistry.
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