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dc.contributor.author정낙신-
dc.contributor.author최원준-
dc.date.accessioned2016-08-28T12:08:54Z-
dc.date.available2016-08-28T12:08:54Z-
dc.date.issued2008-
dc.identifier.issn0960-894X-
dc.identifier.otherOAK-4684-
dc.identifier.urihttps://dspace.ewha.ac.kr/handle/2015.oak/219971-
dc.description.abstractOn the basis of potent and selective A3 adenosine receptor (AR) antagonist, 2-chloro-N6-(3-iodobenzyl)-4′-thioadenosine-5′-N,N-dimethyluronamide, structure-activity relationships were studied for a series of 5′-N,N-dialkyluronamide derivatives, synthesized from d-gulonic γ-lactone. From this study, it was revealed that removal of the hydrogen bond-donating ability of the 5′-uronamide was essential for the pure A3AR antagonism. 5′-N,N-Dimethyluronamide derivatives exhibited higher binding affinity than larger 5′-N,N-dialkyl or 5′-N,N-cycloalkylamide derivatives, indicating that steric factors are crucial in binding to the human A3AR. A N6-(3-bromobenzyl) derivative 6c (Ki = 9.32 nM) exhibited the highest binding affinity at the human A3AR with very low binding affinities to other AR subtypes. © 2008 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.titleStructure-activity relationships of 2-chloro-N6-substituted-4′-thioadenosine-5′-N,N-dialkyluronamides as human A3 adenosine receptor antagonists-
dc.typeArticle-
dc.relation.issue5-
dc.relation.volume18-
dc.relation.indexSCI-
dc.relation.indexSCIE-
dc.relation.indexSCOPUS-
dc.relation.startpage1612-
dc.relation.lastpage1616-
dc.relation.journaltitleBioorganic and Medicinal Chemistry Letters-
dc.identifier.doi10.1016/j.bmcl.2008.01.070-
dc.identifier.wosidWOS:000254180200014-
dc.identifier.scopusid2-s2.0-39849107763-
dc.author.googleJeong L.S.-
dc.author.googleLee H.W.-
dc.author.googleKim H.O.-
dc.author.googleTosh D.K.-
dc.author.googlePal S.-
dc.author.googleChoi W.J.-
dc.author.googleGao Z.-G.-
dc.author.googlePatel A.R.-
dc.author.googleWilliams W.-
dc.author.googleJacobson K.A.-
dc.author.googleKim H.-D.-
dc.contributor.scopusid정낙신(16028528200)-
dc.contributor.scopusid최원준(55732412300;57211762651)-
dc.date.modifydate20230627112239-
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약학대학 > 약학과 > Journal papers
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