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dc.contributor.authorMcKeveney, Declanen_US
dc.contributor.authorQuinn, Ronalden_US
dc.date.accessioned2017-04-24T10:58:03Z
dc.date.available2017-04-24T10:58:03Z
dc.date.issued2000en_US
dc.identifier.issn0968-0896en_US
dc.identifier.doi10.1016/S0968-0896(00)00190-5en_US
dc.identifier.urihttp://hdl.handle.net/10072/3145
dc.description.abstractSubstitution of 1-phenylpyrazolo[3,4-d]pyrimidines at C6 with N-alkyl-2-thiopropionamide groups has resulted in a series of 18 compounds which have been evaluated for binding at A1 and A2A adenosine receptors. Introduction of an N-ethyl group gave increased affinity at both A1 and A2A receptors for the amino compound 7b compared to the primary amide 7a. An additional hydrophobic pocket exists for substituents on the amide. This pocket allows an N-ethyl group for increased affinity at both A1 and A2A receptors, allows larger alkyl groups at A2A receptors but not at A1 receptors and there is an H-bond interaction requiring one H-bond donor. Molecular modeling studies have also enabled a proposal of the amino acid residues involved in ligand binding at both the A1 and A2A receptors.en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_US
dc.languageEnglishen_US
dc.language.isoen_US
dc.publisherPergamonen_US
dc.publisher.placeUKen_US
dc.relation.ispartofpagefrom2581en_US
dc.relation.ispartofpageto2590en_US
dc.relation.ispartofjournalBioorganic & Medicinal Chemistryen_US
dc.relation.ispartofvolume8en_US
dc.subject.fieldofresearchHISTORY AND ARCHAEOLOGYen_US
dc.subject.fieldofresearchcode210000en_US
dc.title1-Phenylpyrazolo[3,4-dlpyrimidines:Structure-Activity Relationships for C6 Substituents at A1 and A2a Adenosine Receptorsen_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.facultyGriffith Sciences, Griffith Institute for Drug Discoveryen_US
gro.date.issued2015-05-04T01:47:34Z
gro.hasfulltextNo Full Text


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