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Synthesis and in vitro stability of nucleoside 5'-phosphonate derivatives.

Abstract
Nucleoside derivatives are largely synthesized and tested to investigate their influence on platelet aggregation. It's well known that P2Y receptors play an important role in the regulation of platelet function and, as consequence, in controlling atherothrombotic events. The research of compounds that antagonize P2Y(1) and, in particular, P2Y(12) receptors is of great interest in the aim to obtain platelet aggregation inhibitors that are effective in the prevention and treatment of arterial thrombosis. In this study we present the synthesis and in vitro metabolic stability in human blood and rat liver homogenate of a new class of nucleoside derivatives, in particular 5'-phosphonate adenosine, inosine, guanosine and thioadenosine analogues also modified at the ribose moiety. On the basis of the results obtained we can hypothesize compounds 4 and 18 to have in vivo a relatively high stability.
AuthorsSilvia Vertuani, Anna Baldisserotto, Katia Varani, Pier Andrea Borea, Bonache De Marcos Maria Cruz, Luca Ferraro, Stefano Manfredini, Alessandro Dalpiaz
JournalEuropean journal of medicinal chemistry (Eur J Med Chem) Vol. 54 Pg. 202-9 (Aug 2012) ISSN: 1768-3254 [Electronic] France
PMID22705000 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier Masson SAS. All rights reserved.
Chemical References
  • Nucleosides
  • Organophosphonates
  • Platelet Aggregation Inhibitors
Topics
  • Animals
  • Chemistry Techniques, Synthetic
  • Drug Stability
  • Humans
  • Liver (metabolism)
  • Male
  • Nucleosides (blood, chemical synthesis, chemistry, metabolism)
  • Organophosphonates (chemistry)
  • Platelet Aggregation Inhibitors (blood, chemical synthesis, chemistry, metabolism)
  • Rats
  • Rats, Wistar

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