Synthesis, Characterization and Erythrocyte Encapsulation of an Azidothymidine Homodinucleotide View Full Text


Ontology type: schema:Chapter     


Chapter Info

DATE

1997

AUTHORS

Marco Giovine , Sonia Scarfi , Anna Gasparini , Enrico Millo , Gianluca Damonte , Antonio De Flora , Mauro Magnani , Alessandra Fraternale , Luigia Rossi , Rosamund Williams , Umberto Benatti

ABSTRACT

A new nucleoside analogue, di(thymidine-3′-azido-2′,3′-dideoxy-D-riboside)-5′-5′-p1-p2-pyrophosphate (AZTp2AZT), was designed and synthesized to overcome some limitations of conventional antiretroviral chemotherapy based upon nucleoside analogues (AZT, ddC, ddI). Indeed, the triphosphorylated form of these nucleoside analogues is able to inhibit the infectivity and replication of Human Immunodeficiency Virus (HIV-1), but the main problems in the use of these drugs concern their limited phosphorylation in some cells (e.g., macrophages) and their cytotoxic side effects. AZTp2AZT was encapsulated in human erythrocytes according to a conservative procedure of hypotonic shock-isotonic resealing and reannealing and showed a remarkable stability and a slow conversion to 5′-monophosphate (AZT-MP) and to AZT. This azidothymidine homodinucleotide seems to have chemical and biochemical properties enabling its profitable utilization in the erythrocyte-encapsulated form. More... »

PAGES

43-50

Book

TITLE

Erythrocytes as Drug Carriers in Medicine

ISBN

978-1-4899-0046-3
978-1-4899-0044-9

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/978-1-4899-0044-9_6

DOI

http://dx.doi.org/10.1007/978-1-4899-0044-9_6

DIMENSIONS

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