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Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4′-thioadenosine derivatives without 4′-hydroxymethyl group as highly potent and selective antagonists

Title
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4′-thioadenosine derivatives without 4′-hydroxymethyl group as highly potent and selective antagonists
Authors
Lak S.J.Seung A.C.Gunaga P.Hea O.K.Hyuk W.L.Sang K.L.Tosh D.K.Patel A.Palaniappan K.K.Gao Z.-G.Jacobson K.A.Hyung R.M.
Ewha Authors
정낙신이상국
Issue Date
2007
Journal Title
Journal of Medicinal Chemistry
ISSN
0022-2623JCR Link
Citation
vol. 50, no. 14, pp. 3159 - 3162
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
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 A3 adenosine receptor (AR), N 6-substituted purine analogues bound potently and selectively and acted as antagonists in a cyclic AMP functional assay. An N6-(3- chlorobenzyl)purine analogue 9b displayed a Ki value of 1.66 nM at the human A3 AR. Thus, truncated D-4′-thioadenosine is an excellent template for the design of novel A3 AR antagonists to act at both human and murine species. © 2007 American Chemical Society.
DOI
10.1021/jm070259t
Appears in Collections:
약학대학 > 약학과 > Journal papers
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