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Design and synthesis of truncated 4'-thioadenosine derivatives as potent and selective A3 adenosine receptor antagonists.

Title
Design and synthesis of truncated 4'-thioadenosine derivatives as potent and selective A3 adenosine receptor antagonists.
Authors
Hou X.Pal S.Choi W.J.Kim H.O.Tipnis A.Jacobson K.A.Jeong L.S.
Ewha Authors
정낙신최원준
Issue Date
2008
Journal Title
Nucleic acids symposium series (2004)
ISSN
1746-8272JCR Link
Citation
no. 52, pp. 641 - 642
Indexed
SCOPUS scopus
Abstract
We have established structure-activity relationships of novel truncated D-4'-thioadenosine derivatives from D-mannose as potent and selective A(3) adenosine receptor (AR) antagonists. At the human A(3) AR, most of N(6)-substituted analogues showed high potency and selectivity and acted as pure antagonists in a cyclic AMP functional assay. Among compounds tested, 2-chloro-N(6)-3-chlorobenzyl and N(6)-3-chlorobenzyl analogues displayed very high binding affinities (K(i) = 1.66 nM and 1.5 nM, respectively) at the human A(3) AR. Truncated 4'-thioadenosine derivatives studied here are regarded as an excellent template for the design of novel A(3) AR antagonists to act at both human and murine species.
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약학대학 > 약학과 > Journal papers
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