Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 14, Pages 3159-3162Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm070259t
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- Intramural NIH HHS [Z01 DK031117-20] Funding Source: Medline
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Truncated D-4'-thioadenosine derivatives lacking the 4'-hydroxymethylene moiety were synthesized starting from D-mannose, using cyclization to the 4-thiosugar and one-step conversion of the diol to the acetate as key steps. At the human A(3) adenosine receptor (AR), N(6)-substituted purine analogues bound potently and selectively and acted as antagonists in a cyclic AMP functional assay. An N(6)-(3-chlorobenzyl)purine analogue 9b displayed a K(i) value of 1.66 nM at the human A(3) AR. Thus, truncated D-4'-thioadenosine is an excellent template for the design of novel A(3) AR antagonists to act at both human and murine species.
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