Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5938
DC FieldValueLanguage
dc.contributor.authorTuccinardi, Ten_us
dc.contributor.authorZizzari, Aten_us
dc.contributor.authorBrullo, Cen_us
dc.contributor.authorDaniele, Sen_us
dc.contributor.authorMusumeci, Fen_us
dc.contributor.authorSchenone, Sen_us
dc.contributor.authorTrincavelli, Mlen_us
dc.contributor.authorMartini, Cen_us
dc.contributor.authorMartinelli, Aen_us
dc.contributor.authorGiorgi, Gianlucaen_us
dc.contributor.authorBotta, Maurizioen_us
dc.date.accessioned2021-03-30T15:56:14Z-
dc.date.available2021-03-30T15:56:14Z-
dc.date.issued2011-
dc.identifier.issn1477-0520en_US
dc.identifier.urihttp://hdl.handle.net/20.500.12779/5938-
dc.description40547en_US
dc.description.abstractA(1) adenosine receptor antagonists have been proposed to possess an interesting range of potential therapeutic applications. We have already reported the synthesis and the biological characterization of a family of pyrazolo[3,4-b]pyridine derivatives as A(1) adenosine ligands endowed with an antagonistic profile. In the present work, we report the LC separation of enantiomers of our most active A(1) antagonists together with the determination of their absolute configuration by means of X-ray crystal structure analysis. Biological assays confirmed a different activity for the two enantiomers, with the R one showing the higher human A(1)AR affinity. We also developed a homology model of this receptor subtype in order to suggest a binding disposition of the ligands into the hA(1)AR. All of the obtained data suggest that the compound's chirality plays a key role in A(1) affinity.en_US
dc.language.isoenen_US
dc.relationNoneen_US
dc.relation.ispartofORGANIC & BIOMOLECULAR CHEMISTRYen_US
dc.titleSubstituted pyrazolo[3,4-b]pyridines as human A1 adenosine antagonists: developments in understanding the receptor stereoselectivity.en_US
dc.typeArticleen_US
dc.identifier.doi10.1039/C0OB01064Ben_US
dc.identifier.pmid21390354en_US
dc.identifier.scopus2-s2.0-79958004240en_US
dc.identifier.isiWOS:000291218900010en_US
dc.relation.volume9en_US
dc.description.firstpage4448en_US
dc.description.lastpage4455en_US
dc.description.thirdmissionNot applicableen_US
item.cerifentitytypePublications-
item.grantfulltextnone-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeArticle-
item.fulltextNo Fulltext-
crisitem.author.orcid0000-0002-8817-7745-
crisitem.author.orcid0000-0003-0456-6995-
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