Data di Pubblicazione:
2014
Citazione:
SYNTHESIS AND DEVELOPMENT OF NEW ANTIBACTERIAL AGENTS INHIBITORS OF FTSZ / G. Chiodini ; tutor: E. Valoti ; coordinator: E. Valoti. DIPARTIMENTO DI SCIENZE FARMACEUTICHE, 2014 Feb 25. 26. ciclo, Anno Accademico 2013. [10.13130/chiodini-giuseppe_phd2014-02-25].
Abstract:
Elements of the bacterial cytoskeleton represent potential targets for antimicrobial compounds. FtsZ (Filamentous temperature sensitive Z) is a bacterial ancestor of eukaryotic tubulin. It possess markedly different structures than its eukaryotic analogue, making possible to develop specific inhibitors for the bacterial protein. The 3-methoxybenzamide (3-MBA) has a weak antibacterial activity against B. subtilis, it can easily penetrate bacterial cell and bind FtsZ at high ligand efficiency. The fluorinated 3-MBA analogue 2,6-difluoro-3-nonyloxybenzamide (compound 1) showed a significant activity against B. subtilis and S. aureus. Starting from the compound 1 we designed and synthesized a new series of derivatives that replaced the amide function with bioisosteric groups and new compounds differently substituted at the 3 position of the 2,6-difluoro-3-hydroxybenzamide.
Tipologia IRIS:
Tesi di dottorato
Elenco autori:
G. Chiodini
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