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Synthesis of N6-alkyl(aryl)-2-alkyl(aryl)thioadenosines as antiplatelet agents.

Abstract：

:A series of novel N(6)-alkyl(aryl)-2-alkyl(aryl)thioadenosines were synthesized, and their human antiplatelet aggregation activities were evaluated by the stimulation of adenosine 5'-diphosphate (ADP). Some of these compounds showed strong activity, among which compound 5b(11) displayed the highest activity with an IC(50) value of 29 ± 3 μM. Furthermore, five compounds were tested against arachidonic acid (AA)-induced human platelet aggregation. The results showed that compound 5b(10) exhibited the highest activity with an IC(50) value of 3 ± 2 μM. The adenosine derivatives substituted with a phenethyl group at the N(6) position and a methylthio or ethylthio group at the C-2 position displayed high antiplatelet aggregation activity.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Liu G,Xu J,Chen N,Zhang S,Ding Z,Du H

doi

10.1016/j.ejmech.2012.03.047

subject

Has Abstract

pub_date

2012-07-01 00:00:00

pages

114-23

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00209-7

journal_volume

53

pub_type

杂志文章

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