Κατεύθυνση Οργανική Σύνθεση και Εφαρμογές της στη Χημική Βιομηχανία
Library of the School of Science

2024-10-30

2024

Papagiorgou Anna-Krinio

Μαγκριώτη Βικτωρία, Αναπληρώτρια Καθηγήτρια, Τμήμα Χημείας, ΕΚΠΑ, (Επιβλέπουσα),
Δημήτριος Γεωργιάδης, Καθηγητής Τμήμα Χημείας, ΕΚΠΑ,
Χριστόφορος Κόκοτος, Καθηγητής Τμήμα Χημείας, ΕΚΠΑ

Σχεδιασμός και σύνθεση β-λακτονών και β-λακταμών ως αντιμυκοβακτηριακές ενώσεις

Greek

Design and synthesis b-lactones and b-lactams as antimycobacterial compounds

Tuberculosis is an infectious and fatal disease caused by Mycobacterium Tuberculosis and is the second leading cause of death from a single infectious agent after COVID-19 infection. The emergence of resistant strains of the mycobacterium to existing drugs and the long-term treatment with known treatment regimens necessitate the need for the development of new anti-tuberculosis drugs.
Beta-lactones are organic molecules consisting of a high angular-tension heterocyclic ring and have emerged as useful and potent enzymatic inhibitors of bacteria and mycobacteria such as M. tuberculosis. At the same time, beta-lactams, which are mainly known for their antibiotic activity, cover a significant part of the pharmaceutical market and are used for the treatment of bacterial infections. Beta-lactams are characterised by the four-membered lactam ring, and the various groups attached to this ring determine the activity, stability and tolerance of the molecule to bacterial enzymes, such as beta-lactamases.
The aim of this present work is the diastereoselective synthesis of β-lactones bearing a medium, or long aliphatic chain, saturated, or unsaturated at the α-position and a small propyl chain at the β-position of the ring. The design and synthesis of α,β-substituted β-lactams bearing a saturated carbon chain at the α-position is also disclosed.

Science

antimycobacterial activity, β-lactones, β-lactams, tuberculosis

No

0

Yes

119

167

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https://pergamos.lib.uoa.gr/uoa/dl/object/3421711