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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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Vertuani S,Baldisserotto A,Varani K,Borea PA,De Marcos Maria Cruz B,Ferraro L,Manfredini S,Dalpiaz A

doi

10.1016/j.ejmech.2012.04.045

subject

Has Abstract

pub_date

2012-08-01 00:00:00

pages

202-9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00298-X

journal_volume

54

pub_type

杂志文章

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