Unit:
Κατεύθυνση Οργανική Σύνθεση και Εφαρμογές της στη Χημική ΒιομηχανίαLibrary of the School of Science
Author:
Pagonis Alexandros
Supervisors info:
Βικτωρία Μαγκριώτη Επίκ. Καθηγήτρια (Επιβλέπουσα), Τμήμα Χημείας, Εθνικό και Καποδιστριακό Πανεπιστήμιο Αθηνών
Γεώργιος Κόκοτος, Καθηγητής, Τμήμα Χημείας, Εθνικό και Καποδιστριακό Πανεπιστήμιο Αθηνών
Δημήτρης Γεωργιάδης Αναπλ. Καθηγητής, Τμήμα Χημείας, Εθνικό και Καποδιστριακό Πανεπιστήμιο Αθηνών
Original Title:
Σχεδιασμός, Σύνθεση και Αντιμυκοβακτηριδιακή Δράση Υδροξαμικών Οξέων και Αναλόγων τους
Translated title:
Design, Synthesis and Antimycobacterial Activity of Hydroxamic Acids and Their Analogues
Summary:
Tuberculosis (TB) is an infectious disease mainly caused by the Mycobacterium Τuberculosis (Mtb) and, according to the World Health Organization (WHO), it is the leading cause of death due to a single infectious agent. One of the first-line drugs for treating TB is isoniazid, the hydrazide of isonicotinic acid. Hydroxamic acids are amides, where the nitrogen bears a hydroxyl group, instead of a hydrogen atom and they are capable inhibitors of various enzymes, such as ureases, peroxidases and metalloproteinases.
In the present thesis, we analyze the design and the synthesis of novel hydroxamic acids, their derivatives and hydrazide analogues for the study of their action against TB. The Mycobacterium tuberculosis properties, the diagnosis and treatment methods of TB, as well as the new emerging, resistant forms of the disease are analyzed, while reference is made to the antibiotics prescribed against TB. Moreover, the biological activity and the synthetic methodologies of hydroxamic acids, cinnamic acids and hydrazides are reported. In the second part we present the synthesis of novel isoniazid analogues, which are hydroxamic acids, hydrazides as well as substituted hydroxamic acids.
Main subject category:
Science
Keywords:
Antimycobacterial activity, Hydrazides, Hydroxamic acids, Tuberculosis
