The antibiotic resistance is a very huge worldwide problem. Multi-drug resistant and opportunistic bacteria lead to infections and deaths especially in immunosuppressive and hospitalized patients, using different strategies to defend itself from the antibiotics. It is therefore necessary develop new efficient compounds against resistant bacteria grouped under the acronymous ESKAPE. In the last decade our investigative group of University of Seville (Faculty of Pharmacy, Department of Organic and Pharmaceutic Chemistry) designed new active compounds characterized by the presence of urea or thiourea functional groups. The aim of this thesis, that was performed in the above mentioned research group inside Erasmus Programme, is the design, the synthesis and the evaluation of new compounds developed by active prototypes powered in earlier studies. Starting from available backbones as serinol, allylamine and 1,3 diamino- 2- propanol, 19 compounds were obtained. Their hypotisized structures were confirmed by Nuclear Magnetic Resonance and Mass Spectrometry. Subsequently, their antibacterial activities were proved against 5 different strains of Gram-positive and Gram-negative bacteria and one type of yeast, thanks to the collaboration with the Department of microbiology and parasitology of the Faculty of Pharmacy of Seville. The compounds have not demonstrated activity but their design and their short and enhanced synthesis have led to useful developments for the investigative group.
Disegno, sintesi e valutazione biologica di librerie di piccole molecole con potenziale attività antimicrobica.
QUAGLIA, LUCREZIA ANNA
2021/2022
Abstract
The antibiotic resistance is a very huge worldwide problem. Multi-drug resistant and opportunistic bacteria lead to infections and deaths especially in immunosuppressive and hospitalized patients, using different strategies to defend itself from the antibiotics. It is therefore necessary develop new efficient compounds against resistant bacteria grouped under the acronymous ESKAPE. In the last decade our investigative group of University of Seville (Faculty of Pharmacy, Department of Organic and Pharmaceutic Chemistry) designed new active compounds characterized by the presence of urea or thiourea functional groups. The aim of this thesis, that was performed in the above mentioned research group inside Erasmus Programme, is the design, the synthesis and the evaluation of new compounds developed by active prototypes powered in earlier studies. Starting from available backbones as serinol, allylamine and 1,3 diamino- 2- propanol, 19 compounds were obtained. Their hypotisized structures were confirmed by Nuclear Magnetic Resonance and Mass Spectrometry. Subsequently, their antibacterial activities were proved against 5 different strains of Gram-positive and Gram-negative bacteria and one type of yeast, thanks to the collaboration with the Department of microbiology and parasitology of the Faculty of Pharmacy of Seville. The compounds have not demonstrated activity but their design and their short and enhanced synthesis have led to useful developments for the investigative group.File | Dimensione | Formato | |
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https://hdl.handle.net/20.500.14240/87064