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Structure-activity relationships of truncated D- and L-4′- thioadenosine derivatives as species-independent A3 adenosine receptor antagonists

Title
Structure-activity relationships of truncated D- and L-4′- thioadenosine derivatives as species-independent A3 adenosine receptor antagonists
Authors
Lak S.J.Pal S.Seung A.C.Won J.C.Jacobson K.A.Gao Z.-G.Klutz A.M.Hou X.Hea O.K.Hyuk W.L.Sang K.L.Tosh D.K.Hyung R.M.
Ewha Authors
정낙신이상국최원준
Issue Date
2008
Journal Title
Journal of Medicinal Chemistry
ISSN
0022-2623JCR Link
Citation
vol. 51, no. 20, pp. 6609 - 6613
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Novel D- and L-4′-thioadenosine derivatives lacking the 4′-hydroxymethyl moiety were synthesized, starting from D-mannose and D-gulonic γ-lactone, respectively, as potent and selective species-independent A3 adenosine receptor (AR) antagonists. Among the novel 4′-truncated 2-H nucleosides tested, a N6-(3- chlorobenzyl) derivative 7c was the most potent at the human A3 AR (Ki = 1.5 nM), but a N6-(3-bromobenzyl) derivative 7d showed the optimal species-independent binding affinity. © 2008 American Chemical Society.
DOI
10.1021/jm8008647
Appears in Collections:
약학대학 > 약학과 > Journal papers
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