Τομέας ΙΙ [Οργανική Χημεία – Οργανική Χημική Τεχνολογία – Χημεία Τροφίμων]
Library of the School of Science

2014-01-23

2014

Μαυρίδης Ιωάννης

Γεωργιάδης Δημητριος Επίκουρος Καθηγητης ΕΚΠΑ (επιβλέπων), Βουρλούμης Διονύσιος Ερευνητής Α΄ ΕΚΕΦΕ "ΔΗΜΟΚΡΙΤΟΣ", Ζωγράφος Αλέξανδρος Επίκουρος Καθηγητής ΑΠΘ

Σύνθεση και μελέτη μη φυσικών δομών που αλληλεπιδρούν με το ριβοσωμικό RNA

Greek

Synthesis and study of unnatural structures that interact with the ribosomic RNA

The bacterial ribosome represents the biological target for a variety of known
antibiotics, aminoglycosides being the most characteristic example. The
pharmaceutical properties of aminoglycosides are due to their ability to bind
strongly to the bacterial A-site. This binding interferes with the mechanism of
protein synthesis and eventually results in cell death. Nevertheless, despite
their former universitality their effectiveness has been greatly diminished by
the increasing appearance of resistant bacterial strains. In this thesis,
aiming to a new generation of antibiotics based on the aminoglycoside
structures, we have designed and synthesized a series of novel, spiro-bicyclic
analogues. Selecting amongst the most promising analogues we proceeded to
further derivatization by means of proper substitution. The resulting second
generation products presented improved antibacterial properties. Furthermore we
envisioned and tested a new protocol for indentifying the binding sites of
small molecules within the RNA target. Being able to apply such a procedure to
molecules with pharmaceutical significance would lead to better clarification
of their mechanism of action and easier synthetic protocols of improved
analogues.

Aminoglucosidic analogues, Antibiotics, Spiroethers, A-Site, RNA

Yes

1-7

Yes

122

200

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https://pergamos.lib.uoa.gr/uoa/dl/object/1309382