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Synthesis and binding affinity of homologated adenosine analogues as A3 adenosine receptor ligands

Title
Synthesis and binding affinity of homologated adenosine analogues as A3 adenosine receptor ligands
Authors
Lee H.W.Choi W.J.Jacobson K.A.Jeong L.S.
Ewha Authors
정낙신최원준
Issue Date
2011
Journal Title
Bulletin of the Korean Chemical Society
ISSN
0253-2964JCR Link
Citation
vol. 32, no. 5, pp. 1620 - 1624
Indexed
SCI; SCIE; SCOPUS; KCI WOS scopus
Abstract
Homologated analogues 3a and 3b of potent and selective A3 adenosine receptor ligands, IB-MECA and dimethyl-IB-MECA were synthesized from commercially available 1-O-acetyl-2,3,5-tri-O-benzoyl-β-Dribofuranose (4) via Co2(CO)8-catalyzed siloxymethylation as a key step. Unfortunately, homologated analogues 3a and 3b did not show significant binding affinities at three subtypes of adenosine receptors, indicating that free rotation, resulting from homologation, induced unfavorable interactions in the binding site of the receptor maybe due to the presence of many conformations.
DOI
10.5012/bkcs.2011.32.5.1620
Appears in Collections:
약학대학 > 약학과 > Journal papers
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