Unit:
ΠΜΣ με ειδίκευση ΣΥΝΘΕΤΙΚΗ ΦΑΡΜΑΚΕΥΤΙΚΗ ΧΗΜΕΙΑLibrary of the School of Science
Supervisors info:
Καθηγήτρια ΕΚΠΑ Νικολαΐς Πουλή (επιβλέπουσα), Καθηγητής ΕΚΠΑ Παναγιώτης Μαράκος, Καθηγητής ΕΚΠΑ Εμμανουήλ Μικρός
Original Title:
Σχεδιασμός, Σύνθεση και Φαρμακολογική Αξιολόγηση Νέων Ιμιδαζο[4,5-c]πυριδινών
Translated title:
Design, Synthesis and Pharmacological Evaluation of New imidazo[4,5-C]pyridines
Summary:
Purines constitute the building blocks of the nucleic acids and participate in
many important cellular processes as well. The transport of purine nucleosides
across the cell membraneis mediated by families of transmembrane transporters
(nucleosidetransportproteins, NTPs), which are divided into the
equilibrativenucleosidetransporters(ENTs) and the
concentrativenucleosidetransporters(CNTs). Unlike their mammalian hosts, most
parasites lack the pathways for de novo purine biosynthesis and rely on salvage
pathways and nucleoside transporters to meet their purine demands. Fungi
possess three families of purine transporters and among them FcyB has been
extensively studied. In this project we present the design and synthesis of a
number of new imidazo[4,5-c]pyridines and their biological evaluation as
inhibitors of FcyB transporter of Aspergillusnidulans. The derivatives were
synthesized from suitably substituted nitropyridines, which were first
substituted with selected amino- or ether groups and then cyclized to provide
the fused ring system. N1 alkyl substituents were finally introduced to result
in the target compounds. The preliminary biological results indicate that
N1-isopropyl or cyclopentyl substitution together with the presence of a
4-N-methylpiperazinyl group is in favor of FcyB inhibitory activity, concerning
this class of compounds. These molecules could serve as useful leads for the
development of more potent inhibitors.
Keywords:
Purine transporters, Imidazopyridines, FcyB
