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Synthesis of 2-chloro-N6-substituted-4'-thioadenosine-5'-N, N-dialkyluronamides as potent and selective A3 adenosine receptor antagonists.

Title
Synthesis of 2-chloro-N6-substituted-4'-thioadenosine-5'-N, N-dialkyluronamides as potent and selective A3 adenosine receptor antagonists.
Authors
Choi W.J.Lee H.W.Hou X.Kim H.O.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. 645 - 646
Indexed
SCOPUS scopus
Abstract
The highly selective A(3) receptor agonist, 4'-thio-Cl-IB-MECA was successfully converted into selective A(3) receptor antagonists by appending a second N-alkyl group on the 5'-uronamide position. This result indicates that the hydrogen bonding ability of the 5'-uronamide is essential for the conformational change required for the receptor activation. Among compounds tested, a N(6)-(3-bromobenzyl) derivative with 5'-dimethyluronamide exhibited the highest binding affinity (K(i) = 9.32 nM) at the human A(3) AR with very low binding affinities to other AR subtypes.
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약학대학 > 약학과 > Journal papers
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