Abstract
On the basis of high binding affinity of 2-hexynyl-N 6- methyladenosine and N 6-substituted-4′-thioadenosine derivatives at the A3 adenosine receptor (AR), novel 2-alkynyl-substituted-N 6-methyl-4′-thioadenosine derivatives, combining the characteristics of two classes of nucleosides were designed and synthesized from D-gulonic γ-lactone via palladium-catalyzed cross coupling reaction as a key step. Among compounds tested, only compound 3b showed moderate binding affinity at the human A3 adenosine receptor without binding affinities at other subtypes.
Original language | English |
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Pages (from-to) | 973-977 |
Number of pages | 5 |
Journal | Archives of Pharmacal Research |
Volume | 31 |
Issue number | 8 |
DOIs | |
State | Published - Aug 2008 |
Keywords
- 2-Alkynyl-substituted-N -methyl-4′-thioadenosine; A adenosine receptor
- Binding affinity
- Diazotization
- Palladium-catalyzed cross coupling